Search Result
Results for "
allosteric modulator
" in MedChemExpress (MCE) Product Catalog:
8
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-150056
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Cannabinoid Receptor
Arrestin
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Neurological Disease
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CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively .
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- HY-147558
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Cannabinoid Receptor
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Others
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CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
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-
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- HY-147559
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Cannabinoid Receptor
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Others
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CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs .
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-
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- HY-150057
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Cannabinoid Receptor
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Others
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CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
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-
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- HY-W837864
-
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Others
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Others
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PDK1 allosteric modulator 1 is a molecule targeting PDK1 with a binding affinity of 8 μM. PDK1 allosteric modulator 1 is able to bind to the PIF pocket of PDK1, potentially affecting the biological activity of this kinase .
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-
-
- HY-120411
-
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Calcium Channel
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Others
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Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels .
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-
-
- HY-159826
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-
-
- HY-103503
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-
-
- HY-119765
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-
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- HY-116067
-
-
-
- HY-147530
-
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mGluR
|
Neurological Disease
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mGluR2 modulator 4 (compound 47) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.8 μM. mGluR2 modulator 4 can be used for researching antipsychotic .
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-
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- HY-103497
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-
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- HY-147528
-
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mGluR
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Neurological Disease
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mGluR2 modulator 2 (compound 2) is a potent, selective and orally bioavailable mGluR2 positive allosteric modulator with an EC50 value of 0.13 μM. mGluR2 modulator 2 can be used for researching antipsychotic .
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-
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- HY-162454
-
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EAAT
|
Neurological Disease
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DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC50 value of 1 nM .
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-
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- HY-159829
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-
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- HY-121806
-
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mAChR
|
Neurological Disease
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VU0486846 is an orally active and selective muscarinic acetylcholine receptor M1 positive allosteric modulator (PAM) .
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-
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- HY-122819
-
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CaSR
|
Cardiovascular Disease
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Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM .
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-
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- HY-168025
-
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Others
|
Neurological Disease
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VU6007496 is a highly selective and CNS penetrant M1 positive allosteric modulator (PAM). VU6007496 shows excellent pharmacokinetics (PK) .
|
-
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- HY-119806
-
|
5-HT Receptor
|
Neurological Disease
|
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. TMPPAA enhances 5-HT-mediated 5-HT3AR signaling .
|
-
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- HY-114863
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THCCC
|
mGluR
|
Neurological Disease
|
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC50 of 1.5 μM) negative allosteric modulator and mGluR3 (EC50 of 8.9 μM) positive allosteric modulator .
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-
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- HY-107423
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iGluR
|
Neurological Disease
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GNE 6901 (compound 40) is a potent GluN2A-selective NMDAR positive allosteric modulator (PAM) with an EC50 of 382 nM .
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-
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- HY-103475
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GABA Receptor
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Neurological Disease
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GS39783 is a positive allosteric modulator (PAM) of GABABR. Positive modulation of the GABABR can be used for the research of Nicotine addiction .
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-
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- HY-110191
-
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mGluR
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Neurological Disease
Cancer
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VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM .
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-
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- HY-159177
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mAChR
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Neurological Disease
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M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .
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-
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- HY-116855
-
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mGluR
|
Neurological Disease
|
TASP0433864 is a selective positive allosteric modulator (PAM) of metabotropic glutamate 2 (mGlu2) receptor with EC50 values of 199 nM and 206 nM against human and rat mGlu2 receptors, respectively. TASP0433864 has antipsychotic activity .
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-
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- HY-120023
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mAChR
|
Neurological Disease
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VU0453595 is a highly selective, systemically active M1 positive allosteric modulator (PAM, EC50=2140 nM) for the research of schizophrenia .
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-
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- HY-103561
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mGluR
|
Neurological Disease
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DCB (3,3′-dichlorobenzaldazine) is an neutral allosteric modulator of themetabotropic glutamate receptor metabotropic glutamate receptor subtype 5 (mGluR5) . DCB blocks the positive allosteric regulation of mGluRs (mGluR5) with the help of 3,3′-difluorobenzaldazine (DFB). DCB shows the negative modulatory effect of 3,3′-dimethoxybenzaldazine (DMeOB) .
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-
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- HY-107682
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-
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- HY-100605
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mGluR
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Others
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VU0483605 is a potent and brain-penetrated mGlu1 receptor positive allosteric modulator (PAM). VU0483605 shows excellent mGlu1 PAM activity at both human and rat, with EC50 values of 390 and 356 nM, respectively .
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-
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- HY-10933
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CX516
2 Publications Verification
BDP 12
|
iGluR
|
Neurological Disease
|
CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI) .
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-
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- HY-103574
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ADX-10059 hydrochloride
|
mGluR
|
Neurological Disease
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Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .
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-
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- HY-143312
-
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GLP Receptor
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Metabolic Disease
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V-0219 (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 can be used for obesity-associated diabetes research .
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-
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- HY-107504
-
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mGluR
|
Neurological Disease
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VU0360172 hydrochloride is a potent and selective mGlu5 receptor positive allosteric modulator (PAM) with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 hydrochloride stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice .
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-
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- HY-145585
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MIJ-821
|
iGluR
|
Neurological Disease
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Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A) .
|
-
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- HY-144291
-
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Dopamine Receptor
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Neurological Disease
|
LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
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-
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- HY-120837
-
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GABA Receptor
|
Neurological Disease
|
PZ-II-029 is a GABAA positive allosteric modulator that selectively binds with high affinity to α6β3γ2. PZ-II-029 shows anti-migraine effects .
|
-
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- HY-117959
-
|
LPL Receptor
|
Inflammation/Immunology
|
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM) .
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-
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- HY-12567
-
VU0483253
|
mAChR
|
Neurological Disease
|
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .
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-
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- HY-120527
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mGluR
|
Neurological Disease
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VU0463841 is a potent, selective and brain-penetrant mGlu5 negative allosteric modulator (NAM) with an IC50 of 13 nM. VU0463841 is ineffective against mGlu1-4 and mGlu7-8. VU0463841 has the potential for the Cocaine addiction research .
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- HY-139091
-
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Taste Receptor
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Others
|
FEMA 4774 is a positive allosteric modulator of taste receptors T1R2 and T1R3, two subunits of the human sweet taste receptor. FEMA 4774 is also used as a sucrose sweetness enhancer .
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-
-
- HY-100979
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HDMPPA
|
mAChR
|
Others
|
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
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-
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- HY-164764
-
|
Estrogen Receptor/ERR
|
Endocrinology
|
ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease .
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-
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- HY-113689
-
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Cannabinoid Receptor
|
Neurological Disease
|
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
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-
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- HY-120428
-
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mGluR
|
Neurological Disease
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VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitory activity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders .
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-
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- HY-118301
-
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GABA Receptor
|
Neurological Disease
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ADX71441 is a potent and selective positive allosteric modulator of the GABAB receptor. ADX71441 is bioavailable after oral administration and is brain penetrant. ADX71441 has the potential for research of anxiety, pain and spasticity .
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-
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- HY-101165
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iGluR
|
Neurological Disease
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Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
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- HY-130630
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mGluR
|
Neurological Disease
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mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
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-
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- HY-121736
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AGI-026
|
Isocitrate Dehydrogenase (IDH)
|
Neurological Disease
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AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
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-
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- HY-A0106
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(-)-Tetramisole
|
nAChR
Parasite
|
Infection
Inflammation/Immunology
Cancer
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Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
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-
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- HY-120576
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VU0405652
|
mAChR
|
Neurological Disease
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ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease .
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- HY-12439
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ML380
1 Publications Verification
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mAChR
|
Neurological Disease
|
ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR .
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- HY-117851
-
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CaSR
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Metabolic Disease
Endocrinology
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AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .
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- HY-117734
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iGluR
|
Neurological Disease
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PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors .
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- HY-114978
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mGluR
PERK
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Neurological Disease
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VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
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- HY-159624
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GABA Receptor
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Neurological Disease
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KK-92A, a blood-brain barrier penetrated GABAB positive allosteric modulator (PAM), suppresses alcohol self-administration and cue-induced reinstatement of alcohol seeking in rats .
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- HY-101165R
-
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iGluR
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Neurological Disease
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Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide, a positive allosteric modulator of AMPA receptors, is used frequently to block the desensitization of both native and heterologously expressed AMPA receptors. Cyclothiazide is known to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current .
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-
- HY-144698
-
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mGluR
|
Neurological Disease
|
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect .
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-
- HY-19630
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VU0463597
|
mGluR
|
Neurological Disease
|
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-A0106R
-
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nAChR
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
Levamisole (Standard) is the analytical standard of Levamisole. This product is intended for research and analytical applications. Levamisole ((-)-Levamisole), an anthelmintic agent with immunomodulatory properties. Levamisole acts as a positive allosteric modulator (PAM) for the α3β2 (EC50=300 μM) and α3β4 (EC50=100 μM) subtype of nAChRs. Orally active .
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- HY-144705
-
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Cannabinoid Receptor
|
Neurological Disease
|
GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
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- HY-129274
-
|
mGluR
|
Neurological Disease
|
RO4988546 is a negative allosteric modulator (NAM) that targets metabotropic glutamate receptors 2 and 3 (mGlu2, mGlu3). RO4988546 can reduce the binding of [ 3h]-LY354740 at the positive binding site, while affecting the receptor's G protein coupling and intracellular signaling. RO4988546 can be used in the development of antidepressants and cognitive enhancers .
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- HY-120645
-
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Opioid Receptor
|
Neurological Disease
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (μ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
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- HY-139897
-
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iGluR
|
Neurological Disease
|
CX 717 is a positive allosteric modulator of AMPA receptor. Antidepressant-like effect. CX 717 can be used for the research of adult attention deficit hyperactivity disorder (ADHD) .
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-
- HY-128575
-
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nAChR
|
Neurological Disease
|
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
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- HY-157998
-
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mGluR
Src
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Others
|
mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
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- HY-116553
-
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Wnt
β-catenin
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Cancer
|
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=−6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .
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- HY-114314
-
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HBV
|
Infection
|
BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly. BA-53038B has antiviral activity for hepatitis B virus (HBV) with an EC50 value of 3.32 μM. BA-53038B can be used for the research of chronic hepatitis B .
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- HY-16716
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RG1662; RO5186582
|
GABA Receptor
|
Neurological Disease
|
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
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- HY-103520
-
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GABA Receptor
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Neurological Disease
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
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- HY-141899
-
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mAChR
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Neurological Disease
|
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent .
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- HY-129636A
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GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
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- HY-120184
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AZ13713945
|
mAChR
|
Neurological Disease
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
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- HY-107506
-
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mGluR
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Neurological Disease
|
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
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-
- HY-129636
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(E)-GABAB receptor antagonist 1
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GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
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-
- HY-124803
-
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GCGR
|
Metabolic Disease
|
GPCR modulator-1 is a negative allosteric modulator of GLP receptor. GPCR modulator-1 has the potential for type 2 diabetes research .
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-
- HY-155628
-
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iGluR
|
Others
|
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases .
|
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- HY-145370
-
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iGluR
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Neurological Disease
|
GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
|
-
- HY-118416
-
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Opioid Receptor
|
Neurological Disease
|
BMS-986124 is a μ-opioid receptor silent allosteric modulator (μ-SAMs). BMS-986124 antagonizes positive allosteric modulator effect of BMS-986122 (µ-OR PAM) .
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-
- HY-147421
-
-
- HY-146117
-
|
P-glycoprotein
|
Cancer
|
P-gp modulator 2 (Compound 27) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
|
-
- HY-146118
-
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P-glycoprotein
|
Cancer
|
P-gp modulator 3 (Compound 37) is a potent, competitive, allosteric P-glycoprotein (P-gp) modulator .
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-
- HY-141832
-
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mGluR
|
Neurological Disease
|
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments .
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-
- HY-101216
-
-
- HY-103668A
-
-
- HY-101858
-
-
- HY-15618
-
M1 receptor modulator
|
mAChR
|
Neurological Disease
|
MK-7622 (M1 receptor modulator) is a muscarinic M1 receptor positive allosteric modulator .
|
-
- HY-122150
-
|
iGluR
|
Neurological Disease
|
AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC50: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory .
|
-
- HY-101845
-
FITM
1 Publications Verification
|
mGluR
|
Cancer
|
FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
|
-
- HY-107507
-
-
- HY-107457
-
|
mGluR
|
Neurological Disease
|
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
|
-
- HY-114269
-
|
nAChR
|
Neurological Disease
|
(-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity .
|
-
- HY-107457A
-
|
mGluR
|
Neurological Disease
|
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes .
|
-
- HY-112788
-
-
- HY-120487
-
-
- HY-159527
-
-
- HY-15476
-
-
- HY-121393
-
|
GABA Receptor
|
Neurological Disease
|
Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
|
-
- HY-163779
-
|
Glucosidase
|
Neurological Disease
|
β-Glucocerebrosidase modulator 1 (Compound 28) is an allosteric modulator for β-Glucocerebrosidase with an EC50 of 9.0 μM and a Kd of 0.050 μM .
|
-
- HY-114589
-
|
Others
|
Others
|
VU0240382 is a metabotropic glutamate receptor subtype 5 modulator whose activity differs depending on whether it has allosteric agonist activity. VU0240382 with allosteric agonist activity can activate mGlu(5) receptors in cell lines, but has no agonist activity in natural systems and has similar efficacy to mGlu(5) modulators without allosteric agonist activity in animal models.
|
-
- HY-160529
-
|
nAChR
|
Neurological Disease
|
α7 nAChR Modulator-2 (Compound 7b) is a α7 nAChR positive allosteric modulator (PAM) with an EC50 of 2.1 μM. α7 nAChR Modulator-2 can be used for the research of cognitive disorders .
|
-
- HY-150067
-
|
Cannabinoid Receptor
|
Metabolic Disease
|
CB1R Allosteric modulator 5, a selective cannabinoid-1 receptor (CB1R) inverse agonist with an IC50 value of 4.2 μM and EC50 value of >10 μM. CB1R Allosteric modulator 5 can be used for the research of metabolic and obesity .
|
-
- HY-124906
-
|
iGluR
|
Neurological Disease
|
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .
|
-
- HY-124393
-
|
mGluR
|
Neurological Disease
|
GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
|
-
- HY-19559
-
VU 0409551
|
mGluR
|
Neurological Disease
|
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
|
-
- HY-121848
-
ML397
|
mGluR
|
Neurological Disease
|
VU0155094 is a positive allosteric modulator with differential activity at the various group III mGluRs .
|
-
- HY-147657
-
|
GABA Receptor
|
Neurological Disease
|
GABAA receptor modulator-2 (Compound 20) is selective, orally active α5-GABAAR negative allosteric modulator (NAM) with a Ki of 4.1 nM. GABAA receptor modulator-2 shows high-metabolic stability and good CNS safety .
|
-
- HY-13058B
-
|
mGluR
|
Neurological Disease
|
(R)-ADX-47273 is a potent mGluR5 positive allosteric modulator, with an EC50 of 168 nM for potentiation .
|
-
- HY-103573
-
|
mGluR
|
Neurological Disease
|
VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM .
|
-
- HY-123433
-
|
mGluR
|
Neurological Disease
|
JNJ-40068782 is a potent positive allosteric modulator of the mGlu2 receptor, with the IC50 of 38 nM .
|
-
- HY-128770
-
|
Dopamine Receptor
|
Neurological Disease
|
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor
positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM) .
|
-
- HY-157958
-
|
nAChR
|
Neurological Disease
|
α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
|
-
- HY-W823500
-
|
GLP Receptor
|
Metabolic Disease
|
GLP-1 Receptor modulator 1 (Compound 7) is a potent GLP-1 receptor positive allosteric modulator. GLP-1 Receptor modulator 1 can be used for the research of obesity and type 2 diabetes .
|
-
- HY-162455
-
|
EAAT
|
Others
|
NA-014 (40) is a selective EAAT2 positive allosteric modulator (PAM), with an EC50 of 3 nM .
|
-
- HY-18162
-
|
mGluR
|
Neurological Disease
|
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
|
-
- HY-16766
-
RO4995819
|
mGluR
|
Neurological Disease
|
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .
|
-
- HY-139044
-
|
mAChR
|
Neurological Disease
|
VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4 .
|
-
- HY-105272
-
R 72063
|
GABA Receptor
|
Neurological Disease
|
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
|
-
- HY-105272A
-
R 72063 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Loreclezole hydrochloride, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors .
|
-
- HY-110122
-
|
mGluR
|
Neurological Disease
|
AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect .
|
-
- HY-121623
-
|
Others
|
Others
|
VU0359516 is a compound that modulates mGluR4 activity, obtained through structure-activity relationship analysis of mGluR4 positive allosteric modulators, with improved potency and efficacy, as well as selectivity for mGluR4.
|
-
- HY-16423
-
Org 9487
|
mAChR
|
Neurological Disease
|
Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR) .
|
-
- HY-14774
-
AAD1566
|
nAChR
|
Cancer
|
Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-14419
-
|
mGluR
|
Neurological Disease
|
TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM .
|
-
- HY-100728
-
|
mGluR
|
Neurological Disease
|
BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 47 nM.
|
-
- HY-119941
-
|
mGluR
|
Neurological Disease
|
VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM .
|
-
- HY-124419
-
|
mGluR
|
Neurological Disease
|
RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM .
|
-
- HY-P5860
-
Micrurotoxin 1
|
GABA Receptor
|
Neurological Disease
|
MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist .
|
-
- HY-103535
-
-
- HY-159509
-
Claziprotamide
|
Others
|
Others
|
Claziprotamidum (Claziprotamide) is a pantothenate kinases 1 and 3 (PanK1 and PanK3) positive allosteric modulator (PAM) .
|
-
- HY-111763
-
-
- HY-147529
-
|
mGluR
|
Neurological Disease
|
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice .
|
-
- HY-21297
-
|
iGluR
|
Neurological Disease
|
3,5-Dihydroxy-2-naphthoic acid is a Naphthoic acid derivative. Naphthoic acid is a NMDA receptor allosteric modulator .
|
-
- HY-125880
-
-
- HY-113346
-
Tetrahydro-11-deoxycorticosterone
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties .
|
-
- HY-103498
-
|
GABA Receptor
|
Neurological Disease
|
Org20599 is a positive allosteric modulator and at higher concentrations direct agonist of GABAA receptor with an EC50 of 1.1 μM .
|
-
- HY-120024
-
-
- HY-155467
-
-
- HY-117611
-
-
- HY-128783
-
|
mAChR
|
Neurological Disease
|
VU0090157 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR). VU0090157 increases the affinity of ACh by binding to the allosteric site. VU0090157 can be used in the study of schizophrenia and Alzheimer's disease .
|
-
- HY-114381
-
|
EAAT
|
Neurological Disease
|
GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM .
|
-
- HY-119687
-
|
GABA Receptor
|
Infection
|
Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm . Bifenazate is a positive allosteric modulator of GABA receptor .
|
-
- HY-W001692
-
DOV 273547
|
GABA Receptor
|
Neurological Disease
|
Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit .
|
-
- HY-163097
-
|
iGluR
|
Neurological Disease
|
ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site .
|
-
- HY-163831
-
|
mGluR
|
Neurological Disease
|
AZ12559322 is a positive allosteric modulator of mGluR2, with the Ki value of 1.31 nM. AZ12559322 can be used in neurological research .
|
-
- HY-169178
-
|
mAChR
|
Cancer
|
VU6016235 is a highly selective, orally available and structurally unique tricyclic M4 muscarinic acetylcholine receptor positive allosteric modulator.
|
-
- HY-149975
-
|
iGluR
|
Neurological Disease
|
AMPA receptor modulator-4, a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (BTD), is an orally active positive allosteric modulator of the AMPA receptors (AMPAR PAMs). AMPA receptor modulator-4 can cross the blood-brain barrier. AMPA receptor modulator-4 increases the cognition performance and improves working memory performance in mice .
|
-
- HY-141839
-
|
GCGR
|
Metabolic Disease
|
GLP-1R modulator C16 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 8.43 ± 3.82 μM).
|
-
- HY-141840
-
|
GCGR
|
Metabolic Disease
|
GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).
|
-
- HY-100366
-
|
mGluR
|
Neurological Disease
|
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor .
|
-
- HY-18654
-
|
mGluR
|
Neurological Disease
|
ADX88178 is a potent metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 4 nM for human mGluR4.
|
-
- HY-12157
-
|
mAChR
|
Others
|
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
|
-
- HY-112814
-
|
mGluR
|
Neurological Disease
|
VU6001376 is a potent and selective positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4 PAM) with an EC50 of 50.1 nM .
|
-
- HY-137204
-
|
GABA Receptor
|
Neurological Disease
|
COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats .
|
-
- HY-16951
-
|
mGluR
|
Neurological Disease
|
VU-1545 is a metabotropic glutamate receptor 5 positive allosteric modulator (mGluR5 PAM) with a Ki of 156 nM and an EC50 of 9.6 nM .
|
-
- HY-119078
-
|
mGluR
|
Neurological Disease
|
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM .
|
-
- HY-122138
-
|
mGluR
|
Neurological Disease
|
VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant .
|
-
- HY-129086
-
|
iGluR
|
Neurological Disease
|
BPAM344 is a kainate receptor (KAR) subunits GluK1b, GluK2a, and GluK3a positive allosteric modulator (PAM) .
|
-
- HY-112781
-
PF-04958242
|
iGluR
|
Neurological Disease
|
Pesampator (PF-04958242) is a potent and highly selective positive allosteric modulator of AMPA receptor (an AMPA potentiator) with an EC50 of 310 nM and a Ki of 170 nM .
|
-
- HY-120375
-
-
- HY-101841
-
|
mAChR
|
Neurological Disease
|
LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor. LY 2033298 can be used in the study of psychiatric disorders .
|
-
- HY-168028
-
|
mGluR
|
Neurological Disease
|
mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC50 of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases .
|
-
- HY-13236
-
-
- HY-13288
-
-
- HY-12509
-
|
iGluR
|
Neurological Disease
|
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.
|
-
- HY-114403
-
|
mGluR
|
Neurological Disease
|
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
|
-
- HY-132806
-
RG-7816; RO-7017773
|
GABA Receptor
|
Neurological Disease
|
Alogabat (example 8) is a GABAA α5 receptor positive allosteric modulators (PAMs) (extracted from patent WO2018104419A1) .
|
-
- HY-103571
-
|
mGluR
|
Neurological Disease
|
VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety .
|
-
- HY-19623
-
|
mGluR
|
Neurological Disease
|
VU0092273 is a potent mGlu5 positive allosteric modulator (PAM) that also binds to the MPEP site, with an EC50 of 0.27 μM .
|
-
- HY-141842
-
|
GCGR
|
Metabolic Disease
|
GLP-1R modulator L7-028 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 11.01 ± 2.73 μM).
|
-
- HY-151899
-
|
Adenosine Receptor
|
Inflammation/Immunology
|
A3AR modulator 1 (MRS8054) is an orally active A3 adenosine receptor (A3AR) (Adenosine Receptor) positive allosteric modulator (PAM). A3AR modulator 1 greatly enhances Cl-IB-MECA-stimulated [ 35S]GTPγS binding Emax .
|
-
- HY-116463
-
-
- HY-100667
-
|
iGluR
|
Neurological Disease
|
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .
|
-
- HY-155088
-
|
mGluR
|
Metabolic Disease
|
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
|
-
- HY-122164
-
|
iGluR
|
Neurological Disease
|
LY-503430 is an orally active AMPA receptor positive allosteric modulator (PAM). LY-503430 can be used for the study of Parkinson's disease .
|
-
- HY-161810
-
|
Adenosine Receptor
|
Others
|
MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists .
|
-
- HY-123667
-
|
mGluR
|
Neurological Disease
|
NCFP is a metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM). NCFP can be used in the study of central nervous system diseases .
|
-
- HY-103491
-
|
iGluR
|
Neurological Disease
|
PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates .
|
-
- HY-17537
-
|
IRE1
|
Cancer
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
|
-
- HY-N2370
-
|
iGluR
LXR
|
Neurological Disease
|
24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
|
-
- HY-129946
-
-
- HY-133555
-
|
mGluR
|
Neurological Disease
|
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
|
-
- HY-14758
-
NG2-73
|
GABA Receptor
|
Neurological Disease
|
Adipiplon (NG2-73) is a selective GABAA receptor positive allosteric modulator. Adipiplon is particularly useful in the research of a variety of central nervous system (CNS) disorders.
|
-
- HY-117408
-
|
mAChR
|
Neurological Disease
|
VU6004256 is a potent and selective M1 muscarinic positive allosteric modulator (PAM) with an EC50 value of 155 nM. VU6004256 has the potential for the research of schizophrenia .
|
-
- HY-129408
-
|
GABA Receptor
|
Neurological Disease
|
SGE-516 is a neuroactive steroid that is a potent positive allosteric modulator of synaptic and extra-synaptic GABAA receptors. SGE-516 has anticonvulsant activity .
|
-
- HY-110285
-
-
- HY-123837
-
|
Dopamine Receptor
|
Neurological Disease
|
MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling .
|
-
- HY-132812
-
CVL-231
|
mAChR
|
Neurological Disease
|
Emraclidine (CVL-231) is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases .
|
-
- HY-124372
-
|
mGluR
|
Neurological Disease
|
JNJ-46356479 is a selective and orally bioavailable mGlu2 receptor positive allosteric modulator (PAM), with the EC50 of 78 nM. JNJ-46356479 shows active in vivo .
|
-
- HY-161113
-
|
CaSR
|
Metabolic Disease
|
Z8554052021 (compound 2021) is a potent CaSR and indeed GPCR positive allosteric modulator (PAM) with an EC50 of 3.3 nM. Z8554052021 has the potential for hyperparathyroidism research .
|
-
- HY-139580
-
CAD-9303
|
iGluR
|
Neurological Disease
|
Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system ..
|
-
- HY-14774S
-
|
nAChR
|
Cancer
|
(Rac)-Monepantel-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-137986
-
|
Potassium Channel
|
Inflammation/Immunology
|
LUF7244 is a selective allosteric modulator of Kv11.1 channels. LUF7244 inhibits early afterdepolarizations. LUF7244 can be used for anti-arrhythmia research .
|
-
- HY-12149
-
|
nAChR
|
Neurological Disease
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM .
|
-
- HY-15393
-
|
mGluR
|
Neurological Disease
|
VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes .
|
-
- HY-108703
-
PXT002331
|
mGluR
|
Neurological Disease
|
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM . Antiparkinsonian effect .
|
-
- HY-107409
-
|
iGluR
|
Neurological Disease
|
GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
|
-
- HY-107498
-
|
iGluR
|
Neurological Disease
|
GNE-8324 is a selective GluN2A positive allosteric modulator. GNE-8324 selectively enhances NMDA receptor (NMDAR)-mediated synaptic responses in inhibitory but not excitatory neurons .
|
-
- HY-14774S1
-
|
nAChR
|
Cancer
|
(Rac)-Monepantel sulfone-d5 is deuterium labeled Monepantel. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-162662
-
|
Cytochrome P450
mAChR
|
Neurological Disease
|
VU6008677 is a positive allosteric modulator (PAM) for M4, with EC50 of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-118179
-
|
Others
|
Neurological Disease
|
VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
|
-
- HY-120068
-
|
mGluR
|
Neurological Disease
|
VU0418506 is a selective positive allosteric modulator of mGlu4, with EC50 values of 68 nM and 46 nM for hmGlu4 and rmGlu4, respectively. VU0418506 exhibits antiparkinsonian activity .
|
-
- HY-124622
-
|
GCGR
|
Metabolic Disease
|
NNC-0640 is an effective negative allosteric modulator (NAM) of the human glucagon receptor (GCGR), with an IC50 value of 69.2 nM. NNC-0640 holds potential for research in the field of diabetes .
|
-
- HY-110278
-
|
mGluR
|
Neurological Disease
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .
|
-
- HY-P1125
-
4-CMTB
4 Publications Verification
|
Free Fatty Acid Receptor
|
Others
|
4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38) .
|
-
- HY-131941
-
|
GABA Receptor
|
Neurological Disease
|
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
|
-
- HY-113346S
-
Tetrahydro-11-deoxycorticosterone-d3
|
Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
|
-
- HY-115575
-
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment .
|
-
- HY-119772
-
ML137
|
Cholinesterase (ChE)
|
Neurological Disease
|
VU0366369 (ML137) is a selective positive allosteric modulator (PAM) for mAChR M1 with an EC50 of 830 nM. VU0366369 can be used in research about central nervous system diseases .
|
-
- HY-14774R
-
|
nAChR
|
Cancer
|
Monepantel (Standard) is the analytical standard of Monepantel. This product is intended for research and analytical applications. Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
|
-
- HY-169345
-
|
mGluR
|
Neurological Disease
|
VU6043653 is a potent, selective and cross the blood-brain barrier metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 value of 325 nM for h mGlu5 .
|
-
- HY-16940
-
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
|
-
- HY-108337
-
|
iGluR
|
Neurological Disease
|
GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively .
|
-
- HY-108703A
-
PXT002331 (monohydrochloride)
|
mGluR
|
Neurological Disease
|
Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM . Antiparkinsonian effect .
|
-
- HY-10167A
-
R-568 hydrochloride
|
CaSR
|
Others
|
Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca 2+ .
|
-
- HY-113320
-
5β-Androsterone
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity . Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form .
|
-
- HY-120567
-
ML182
|
mGluR
|
Neurological Disease
|
VU0400195 (ML182) is a oral active and allosteric modulator of the metabotropic glutamate receptor 4 (mGlu4) with the EC50 of 291 nM. VU0400195 can be used for study of antiparkinsonian animal model .
|
-
- HY-14866
-
ADX-10059
|
mGluR
|
Neurological Disease
|
Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .
|
-
- HY-116236
-
LY2607540
|
Others
|
Others
|
THIIC (LY2607540) is a compound with anxiolytic and antidepressant potential. It is a positive allosteric modulator of mGlu? receptors, exhibits anxiolytic and antidepressant-like activities in multiple animal models, and can also affect sleep and neurochemical changes.
|
-
- HY-10167
-
R-568
|
CaSR
|
Others
|
Tecalcet (R 568), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet (R 568) increases the sensitivity to activation by extracellular Ca 2+ .
|
-
- HY-111332
-
|
mGluR
|
Others
|
(E)-PHCCC is a positive allosteric modulator (PAM) for mGluR4, that enhances the activity of the receptor's endogenous ligand (glutamate), and exhibits activity in the calcium mobilization assay in CHO cells with an EC50 of 3.2 μM .
|
-
- HY-117697
-
|
Others
|
Others
|
Lu AF11205 is a mGlu5 receptor positive allosteric modulator with activity modulating mGlu5 receptor activity. Optimization of Lu AF11205 resulted in a series of potent fused thiazole analogs whose structures and activities were influenced by substituents and which could affect receptor function in cell lines expressing mGlu5 receptors.
|
-
- HY-12151
-
NSC 213859
|
nAChR
|
Neurological Disease
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
|
-
- HY-108710
-
|
mGluR
|
Neurological Disease
|
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .
|
-
- HY-120530
-
|
mGluR
|
Neurological Disease
|
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
|
-
- HY-129527
-
|
iGluR
|
Neurological Disease
|
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity .
|
-
- HY-107111
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
GSK1034702 is a M1 mAChR allosteric agonist. GSK1034702 shows procognitive effects in rodents. GSK1034702 modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction .
|
-
- HY-110145
-
|
TRP Channel
|
Cancer
|
MRS 1477, a dihydropyridine derivative, is a positive allosteric modulator of TRPV1 in the presence of capsaicin. MRS 1477 itself does not induce apoptosis, but the co-existence of MRS 1477 and capsaicin can induce apoptosis .
|
-
- HY-107505
-
|
mGluR
|
Neurological Disease
|
CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC50: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease .
|
-
- HY-119687R
-
|
GABA Receptor
|
Infection
|
Bifenazate (Standard) is the analytical standard of Bifenazate. This product is intended for research and analytical applications. Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm . Bifenazate is a positive allosteric modulator of GABA receptor .
|
-
- HY-107111A
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
GSK1034702 hydrochloride is a M1 mAChR allosteric agonist. GSK1034702 hydrochloride shows procognitive effects in rodents. GSK1034702 hydrochloride modulates hippocampal function to improve memory encoding in nicotine abstinence model of cognitive dysfunction .
|
-
- HY-116205
-
|
Others
|
Others
|
UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
|
-
- HY-15786
-
|
Others
|
Neurological Disease
|
SGE-201 is an allosteric modulator of N-methyl-D-aspartate receptors (NMDARs), demonstrating significant neuroprotective effects by enhancing NMDAR-mediated responses while differing in action among various blockers in neuronal networks.
|
-
- HY-139644
-
|
Adenosine Receptor
|
Neurological Disease
|
MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine .
|
-
- HY-122190
-
|
mAChR
|
Neurological Disease
|
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM .
|
-
- HY-124867
-
|
TSH Receptor
|
Endocrinology
|
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro .
|
-
- HY-157421
-
|
NAMPT
|
Others
|
Nampt activator-4 is a positive allosteric modulator (N-PAM) of nicotinamide phosphoribosyltransferase (NAMPT) with an EC50 of 0.058 μM. Nampt activator-4 can enhance the nicotinamide adenine dinucleotide (NAD +) in cells .
|
-
- HY-107505A
-
|
mGluR
|
Neurological Disease
|
CBiPES is a potent mGlu2 positive allosteric modulator with an EC50 value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases .
|
-
- HY-12629
-
PF-06297470
|
Others
|
Others
|
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies.
|
-
- HY-107663
-
Pro-Leu-Gly-NH2; Melanostatin
|
Dopamine Receptor
|
Neurological Disease
|
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-163532
-
|
Sirtuin
|
Infection
|
FLS-359 is a selective, orally active allosteric modulator for sirtuin 2, with the IC50 of 3 μM. FLS-359 exhibits antiviral activity against RNA and DNA virus, through inhibition of DNA/RNA replication .
|
-
- HY-12324
-
|
Dopamine Receptor
|
Neurological Disease
|
SB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
|
-
- HY-107774
-
|
iGluR
|
Neurological Disease
|
BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
|
-
- HY-101281
-
|
mAChR
|
Neurological Disease
|
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .
|
-
- HY-107198
-
|
GABA Receptor
|
Neurological Disease
|
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface .
|
-
- HY-135891
-
|
CCR
|
Neurological Disease
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-14417
-
|
mGluR
|
Neurological Disease
|
VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
|
-
- HY-P1397
-
|
Cannabinoid Receptor
|
Neurological Disease
|
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .
|
-
- HY-14417B
-
|
mGluR
|
Neurological Disease
|
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
|
-
- HY-116273
-
|
Phospholipase
|
Cancer
|
ML299 is a selective allosteric modulator and a dual inhibitor of phospholipases D1 and D2 (IC50 values are 6 and 12 nM, respectively). ML299 decreases invasive migration in U87-MG glioblastoma cells .
|
-
- HY-120699
-
|
mGluR
|
Neurological Disease
|
RO5488608 is a negative allosteric metabotropic modulator of glutamate receptor 2/3. RO5488608 inhibits LY354740 (HY-18941)-induced intracellular Ca 2+ release and can be used for study of antidepressant .
|
-
- HY-12508
-
|
iGluR
|
Neurological Disease
|
CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
|
-
- HY-13058
-
|
mGluR
|
Neurological Disease
|
ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities .
|
-
- HY-112209
-
|
mAChR
|
Neurological Disease
|
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
|
-
- HY-116819
-
|
GCGR
|
Metabolic Disease
|
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
|
-
- HY-141515
-
|
Opioid Receptor
|
Neurological Disease
|
BMS-986121 is a positive allosteric modulator (PAM) of the μ opioid receptor extracted from patent WO2014107344. BMS-986121 is built on a chemical scaffold representing a new chemotype for μ receptor PAMs .
|
-
- HY-150018
-
|
mAChR
|
Neurological Disease
|
N-Demethyl MK-6884 (compound 34) is a potent M4 mAChR allosteric modulator. N-Demethyl MK-6884 can be used in the studies of alzheimer's disease and other diseases mediated by the M4 mAChR .
|
-
- HY-116819A
-
|
GCGR
|
Metabolic Disease
|
VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM .
|
-
- HY-120004
-
|
mAChR
|
Infection
|
PF-06827443 is a potent, low-clearance, orally bioavailable, and CNS-penetrant M1-selective positive allosteric modulator (PAM) with minimal agonist activity. PF-06827443 induce cholinergic AEs and convulsion .
|
-
- HY-118022
-
|
mGluR
|
Neurological Disease
|
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
|
-
- HY-101281A
-
|
mAChR
|
Neurological Disease
|
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration .
|
-
- HY-131004
-
|
Cannabinoid Receptor
|
Neurological Disease
|
CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain .
|
-
- HY-109160
-
CAD-1883
|
Potassium Channel
|
Neurological Disease
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA) .
|
-
- HY-103572
-
|
mGluR
|
Neurological Disease
|
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC50s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .
|
-
- HY-160888
-
|
mAChR
|
Others
|
ASP8302 is a positive allosteric modulator of muscarinic M3 Receptor. ASP8302 improves voiding efficiency and reduced residual urine volume in two voiding dysfunction models. ASP8302 can be used for research of underactive bladder .
|
-
- HY-107663A
-
Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
|
Dopamine Receptor
|
Neurological Disease
|
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
|
-
- HY-10933S
-
BDP 12-d10
|
Isotope-Labeled Compounds
iGluR
|
Neurological Disease
|
CX516-d10 is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI)[1].
|
-
- HY-110180
-
|
mGluR
|
Neurological Disease
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
|
-
- HY-143312A
-
|
GLP Receptor
|
Metabolic Disease
|
V-0219 hydrochloride (Compound 9) is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). V-0219 hydrochloride can be used for obesity-associated diabetes research .
|
-
- HY-14612
-
|
mGluR
|
Neurological Disease
|
CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
|
-
- HY-14569
-
CDPPB
1 Publications Verification
|
mGluR
|
Neurological Disease
|
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents .
|
-
- HY-117450
-
|
Others
|
Others
|
VU0415374 is a positive allosteric modulator that modulates mGlu4 receptor activity. VU0415374 could help achieve precise light control of physiological responses. VU0415374 has high selectivity and can be used to further study the role of mGlu4 in co-expression of other mGlu receptor systems. The improved properties of VU0415374 make it an important candidate for studying mGlu4 with high precision in space and time .
|
-
- HY-15446
-
RG7090; CTEP Derivative
|
mGluR
|
Neurological Disease
|
Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM . Basimglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-114933
-
|
mAChR
|
Metabolic Disease
|
VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity .
|
-
- HY-113608
-
|
Adenosine Receptor
|
Neurological Disease
|
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain .
|
-
- HY-156634
-
NYX-783
|
iGluR
|
Neurological Disease
|
Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease .
|
-
- HY-155810
-
|
iGluR
|
Neurological Disease
|
DQP-26 is a potent NMDAR negative allosteric modulator with IC50 values of 0.77 μM and 0.44 μM for GluN2C and GluN2D, respectively. DQP-26 has the potential for NMDAR-associated neurological disease research .
|
-
- HY-16579
-
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-16579A
-
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-113320S
-
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Etiocholanolone-d5 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2].
|
-
- HY-143878
-
-
- HY-133862
-
-
- HY-153193
-
|
GLP Receptor
|
Metabolic Disease
|
LSN3160440 is an allosteric modulator of GLP-1R, which acts as a protein–protein interaction (PPI) stabilizer or molecular glue to assist in the adhesion of inactive GLP-1 (9-36) NH2 on GLP-1R .
|
-
- HY-162663
-
ML253
|
mAChR
|
Neurological Disease
|
VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic .
|
-
- HY-169329
-
|
PINK1/Parkin
E1/E2/E3 Enzyme
|
Neurological Disease
|
BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC50: 0.17 μM) .
|
-
- HY-128584
-
AZN-00016130
|
mAChR
|
Neurological Disease
|
VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively. Used in the research of neuropsychiatric disorders .
|
-
- HY-116463D
-
|
Sigma Receptor
|
Neurological Disease
|
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders .
|
-
- HY-10936
-
|
iGluR
|
Neurological Disease
|
S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests .
|
-
- HY-15831
-
-
- HY-113320S1
-
5β-Androsterone-d2
|
Isotope-Labeled Compounds
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
Etiocholanolone-d2 is the deuterium labeled Etiocholanolone. Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity[1]. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form[2][3].
|
-
- HY-143879
-
-
- HY-115796
-
|
Others
|
Others
|
VU0477886 is a metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator with potent activating activity on mGlu4 (EC50 = 95nM, 89% Glu Max), good pharmacokinetic characteristics (brain: plasma Kp = 1.3), and significant therapeutic efficacy in Parkinson's disease models.
|
-
- HY-103423
-
|
Dopamine Receptor
|
Neurological Disease
|
PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists .
|
-
- HY-107509
-
|
mGluR
|
Neurological Disease
|
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .
|
-
- HY-156626
-
NYX-458; NYX-3054
|
iGluR
|
Neurological Disease
|
Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease .
|
-
- HY-110012
-
|
Adenosine Receptor
|
Infection
|
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
|
-
- HY-107651
-
|
mAChR
|
Metabolic Disease
|
VU 0365114 is a selective mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM, and >30 μM for M1, M2, M3 and M4 receptors. VU 0365114 increases insulin secretion stimulated by ACh in human β-cells .
|
-
- HY-14611
-
DFB
|
mGluR
|
Neurological Disease
|
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
|
-
- HY-120613
-
|
Opioid Receptor
|
Neurological Disease
|
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM) .
|
-
- HY-103502
-
CGP7930
1 Publications Verification
|
GABA Receptor
|
Neurological Disease
|
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .
|
-
- HY-118342
-
|
mAChR
|
Neurological Disease
|
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease .
|
-
- HY-103575A
-
|
mGluR
|
Neurological Disease
|
MFZ 10-7 hydrochloride is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5 . MFZ 10-7 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-119226
-
|
mAChR
|
Neurological Disease
|
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
|
-
- HY-110168
-
|
nAChR
|
Neurological Disease
|
NS9283 is a positive positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors. NS9283 can be used in a series of neurological conditions such as attention deficit hyperactivity disorder (ADHD), schizophrenia, Parkinson's disease and Alzheimer's disease .
|
-
- HY-120717
-
|
mGluR
|
Others
|
VU6001966 (compound 15m) is a potent and cross the blood-brain barrier mGlu2 (metabotropic glutamate receptor 2) negative allosteric modulator with IC50s of 78 nM and >30 µM for mGlu2 and mGlu3, respectively. VU6001966 can serve as an mGlu2 PET tracer .
|
-
- HY-103575
-
|
mGluR
|
Neurological Disease
|
MFZ 10-7 is a highly potent and selective mGluR5 NAM (negative allosteric modulator), with a Ki of 0.67 nM for rat mGluR5 . MFZ 10-7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-123904
-
|
iGluR
|
Neurological Disease
|
UoS12258 is a selective positive allosteric modulator of AMPA receptor. UoS12258 enhances AMPA receptor‐mediated synaptic transmission. UoS12258 improves performance in cognition rat models, including Scopolamine (HY-N0296)‐impaired rats and water maze learning and retention in aged rats .
|
-
- HY-121140
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
AZ1729 is a potent free fatty acid 2 receptor (FFA2) activator, acting as a direct allosteric agonist and as a positive allosteric modulator. AZ1729 increases the activity of the endogenously produced short chain fatty acid propionate in Gi-mediated pathways, but not at those transduced by Gq/G11. AZ1729 induces inhibition of isoproterenol-induced lipolysis in mouse adipocytes. AZ1729 also can Induce migration of human neutrophils. AZ1729 can be used for researching the signaling pathways of the physiological roles of FFA2 .
|
-
- HY-124984
-
|
mGluR
|
Neurological Disease
|
ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a agent blocker . ML353 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-158185
-
|
GABA Receptor
|
Others
|
Isocycloseram is an isoxazoline insecticide and acaricide widely recognized as an allosteric modulator of GABA-gated chloride channels. Isocycloseram is active against Lepidopteran, Hemiptera, Coleoptera, Thysanoptera and Diptera pests. Isocycloseram targets the invertebrate Rdl GABA receptor, but the G335M mutation in the third transmembrane domain of the Rdl GABA receptor may mediate resistance .
|
-
- HY-15748
-
ADX-71149
|
mGluR
|
Neurological Disease
|
JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. JNJ-40411813 has orally bioactivity and penetrate the blood-brain barriers. JNJ-40411813 has the potential property of anti-depression .
|
-
- HY-12158
-
|
mAChR
|
Neurological Disease
|
VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively .
|
-
- HY-134494
-
|
GPR68
|
Neurological Disease
|
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
|
-
- HY-19888
-
|
P2X Receptor
|
Inflammation/Immunology
|
GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases .
|
-
- HY-118256
-
|
mGluR
|
Neurological Disease
|
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research .
|
-
- HY-120727
-
|
mGluR
|
Neurological Disease
|
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .
|
-
- HY-122647
-
VU0652957; VU2957
|
mGluR
|
Neurological Disease
|
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease .
|
-
- HY-155672
-
|
5-HT Receptor
|
Neurological Disease
|
JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
|
-
- HY-124821
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .
|
-
- HY-14418
-
ML-128
|
mGluR
|
Neurological Disease
|
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research .
|
-
- HY-16579AS2
-
|
GABA Receptor
|
Neurological Disease
|
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents[1][2][3].
|
-
- HY-12150
-
CCMI
1 Publications Verification
AVL-3288; UCI-4083
|
nAChR
|
Neurological Disease
|
CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
|
-
- HY-103320A
-
|
CaSR
|
Metabolic Disease
|
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-126327
-
|
Histone Methyltransferase
|
Cancer
|
UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-122559
-
|
mGluR
|
Neurological Disease
|
BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
|
-
- HY-131019
-
|
mGluR
|
Neurological Disease
|
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals .
|
-
- HY-103524
-
(-)-Valerenic Acid
|
GABA Receptor
5-HT Receptor
|
Neurological Disease
|
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
|
-
- HY-103320
-
|
CaSR
|
Metabolic Disease
|
Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-126158
-
|
Dopamine Transporter
Serotonin Transporter
|
Neurological Disease
|
SRI-29574 is an allosteric modulator of the dopamine transporter (DAT). SRI-29574 partially inhibits the uptake of the DAT (IC50=2.3 nM) and also partially inhibits the uptake of the serotonin transporter (SERT) and norepinephrine transporter (NET). SRI-29574 may serve as a useful probe to study the function and regulatory mechanisms of DAT .
|
-
- HY-100939
-
|
Sodium Channel
|
Neurological Disease
|
4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
|
-
- HY-13340
-
VU152100
|
mAChR
|
Neurological Disease
|
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
|
-
- HY-16636
-
|
mGluR
|
Neurological Disease
|
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-115864
-
TAK-653; NBI-1065845
|
iGluR
Lipoxygenase
|
Neurological Disease
|
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
|
-
- HY-126327A
-
|
Histone Methyltransferase
|
Cancer
|
UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
|
-
- HY-143312D
-
|
GLP Receptor
|
Metabolic Disease
|
(R)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R .
|
-
- HY-156331
-
|
mGluR
|
Neurological Disease
|
VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
|
-
- HY-16579AR
-
|
GABA Receptor
|
Neurological Disease
|
Etifoxine (Standard) is the analytical standard of Etifoxine. This product is intended for research and analytical applications. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
|
-
- HY-162735
-
|
Others
|
Inflammation/Immunology
|
BRD5080 is a potent GPR65 positive allosteric modulator. BRD5080 induces GPR65-dependent cAMP production. BRD5080 exhibits a robust induction of cAMP activity and recruits G protein for the WT and variant hGPR65 as well as for the mouse ortholog. BRD5080 has the potential for autoimmune and inflammatory diseases research .
|
-
- HY-119082A
-
|
Others
|
Others
|
VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-119256
-
|
Others
|
Neurological Disease
|
COR627 is a GABA receptor positive allosteric modulator with the ability to enhance GABA activity. COR627 exhibits effects on GABA and baclofen stimulation in rat cortical membranes and can increase its affinity for GABA(B) receptors. In vivo experiments have shown that COR627 can enhance the sedative/hypnotic effects of baclofen at pretreatment ineffective doses .
|
-
- HY-149453
-
|
Guanylate Cyclase
|
Cardiovascular Disease
|
MCUF-651 is an orally active guanylyl cyclase A receptor (GC-A) positive allosteric modulator (PAM) (KD: 397 nM ). MCUF-651 binds to GC-A and selectively enhances the binding of atrial natriuretic peptide (ANP) to GC-A. MCUF-651 enhances ANP-mediated cGMP generation in human cardiac, renal, and fat cells. MCUF-651 inhibits cardiomyocyte hypertrophy .
|
-
- HY-14859
-
ADX48621
|
mGluR
|
Neurological Disease
|
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo . Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P1397A
-
|
Cannabinoid Receptor
|
Cardiovascular Disease
|
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
-
- HY-110190
-
ML396
|
mGluR
|
Neurological Disease
|
VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice .
|
-
- HY-105115
-
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
|
-
- HY-143312B
-
|
GLP Receptor
|
Metabolic Disease
|
(R)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (R)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R .
|
-
- HY-123801
-
GL-II-93
|
GABA Receptor
|
Others
|
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
|
-
- HY-12152
-
NSC 216666
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research .
|
-
- HY-15469
-
|
P2X Receptor
|
Neurological Disease
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
|
-
- HY-102070
-
|
Potassium Channel
|
Neurological Disease
|
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias .
|
-
- HY-116463A
-
|
Sigma Receptor
|
Neurological Disease
|
(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
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-
- HY-116463B
-
|
Sigma Receptor
|
Neurological Disease
|
(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
|
-
- HY-116463C
-
|
Sigma Receptor
|
Neurological Disease
|
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders .
|
-
- HY-15470
-
|
P2X Receptor
|
Neurological Disease
|
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
|
-
- HY-103118
-
|
5-HT Receptor
Apoptosis
|
Neurological Disease
Cancer
|
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively .
|
-
- HY-123671
-
|
Neuropeptide Y Receptor
|
Neurological Disease
|
CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy .
|
-
- HY-155484
-
|
Sigma Receptor
|
Neurological Disease
|
SOMCL-668 is a selective and potent sigma-1 receptor allosteric modulator. ?SOMCL-668 shows positive modulation of improvement in social deficits and cognitive impairment induced by the selective sigma-1 agonist PRE084.?SOMCL-668 displays anti-seizure activities and can be used for psychotic illness research .
|
-
- HY-163280
-
|
NAMPT
|
Neurological Disease
|
JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
|
-
- HY-158627
-
|
Others
|
Others
|
JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
|
-
- HY-120783
-
|
Endogenous Metabolite
|
Neurological Disease
|
Lu AF58801 is a potent, orally available, brain-penetrant positive allosteric modulator of α7 nicotinic acetylcholine receptors with efficacy in a novel object recognition task in mice. Lu AF58801 was shown to selectively enhance the activity of α7 nicotinic acetylcholine receptors. Lu AF58801 was able to improve cognitive function in mice treated with subchronic fluchlorothiazol (PCP) .
|
-
- HY-124634
-
PZ-2891
1 Publications Verification
|
Others
|
Neurological Disease
|
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively .
|
-
- HY-107508
-
|
mGluR
|
Neurological Disease
|
VU-29 is a positive allosteric modulator of metabotropic glutamate 5 (mGlu5) receptor (EC50=9 nM and Ki=244 nM for rmGluR5). VU-29 is selective for mGluR5 relative to other mGluR subtypes (EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM) .
|
-
- HY-122255
-
|
mGluR
|
Neurological Disease
|
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
|
-
- HY-120589
-
|
mGluR
|
Neurological Disease
|
VU0360172 is a potent and selective mGlu5 receptor positive allosteric modulator with an EC50 value of 16 nM and a Ki of 195 nM, respectively. VU0360172 stimulates polyphosphoinositide (PI) hydrolysis in vivo, which is abrogated in mGlu5 receptors gene deleted mice . VU0360172 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-148867
-
2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl
|
Dopamine Receptor
|
Neurological Disease
|
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD) .
|
-
- HY-123934
-
|
P-glycoprotein
|
Neurological Disease
|
VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity .
|
-
- HY-108204
-
THRX 918661
|
Others
|
Others
|
AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
|
-
- HY-119082
-
|
Others
|
Others
|
(E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-100403
-
Ro 67-7476
Maximum Cited Publications
10 Publications Verification
|
mGluR
|
Cancer
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist?and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
|
-
- HY-145196
-
|
Cannabinoid Receptor
|
Neurological Disease
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .
|
-
- HY-161296
-
|
Bacterial
HIV
|
Infection
|
TH6342 is a SAMHD1 modulator that binds to pretetrameric SAMHD1 and prevents its oligomerization and allosteric activation. SAMHD1 is a dNTP triphosphohydrolase and an HIV-1 restriction factor. SAMHD1 can limit the replication of retroviruses and DNA viruses and has antiviral effects. The inhibitory mechanism of TH6342 does not occupy the SAMHD1 nucleotide-binding pocket, gently binds the target, and functions as a chemical probe .
|
-
- HY-119282
-
|
mGluR
|
Neurological Disease
|
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
|
-
- HY-103524R
-
(-)-Valerenic Acid (Standard)
|
5-HT Receptor
GABA Receptor
|
Neurological Disease
|
Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
|
-
- HY-12153
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
JNJ-1930942 is a selective and blood-brain barrier (BBB) penetrant α(7) nAChR positive allosteric modulator.JNJ-1930942 enhances the Choline (HY-B0282)-evoked rise in intracellular Ca 2+ levels and neurotransmission at hippocampal dentate gyrus synapses. JNJ-1930942 reverses the naturally occurring sensory gating deficit in DBA/2 mice .
|
-
- HY-124569
-
|
iGluR
|
Neurological Disease
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
|
-
- HY-13456
-
|
iGluR
|
Neurological Disease
|
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases .
|
-
- HY-110152
-
|
mGluR
|
Neurological Disease
|
LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-118140
-
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
|
-
- HY-103552
-
|
mGluR
|
Neurological Disease
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
|
-
- HY-P99171
-
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
- HY-141848A
-
|
mGluR
|
Neurological Disease
|
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor . BMS-984923 is a potent mGluR5 silent allosteric modulator . (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-111161
-
|
nAChR
Parasite
|
Infection
|
GSK575594A is a modulator of the nicotinic acetylcholine receptor (nAChR) in Ascaris suum. GSK575594A enhances muscle contractions induced by acetylcholine (ACh) by binding to the allosteric binding site between subunits within the transmembrane domain of nAChR. At a concentration of 3 μM, GSK575594A significantly increased the contraction induced by ACh in Ascaris suum (Emax increased from 1.19 g to 1.51 g). GSK575594A may be used in research within the field of antiparasitic studies .
|
-
- HY-116149
-
|
Others
|
Others
|
A-424274 is a positive allosteric modulator of the α4β2 neuronal nicotinic acetylcholine receptor with activity to enhance the efficacy of analgesics. A-424274 selectively enhances the potency of a range of nicotinic acetylcholine receptor agonists at the α4β2 receptor and, in preclinical models, co-administration with an α4β2 PAM significantly enhances the analgesic efficacy of ABT-594 at clinically well-tolerated doses in humans.
|
-
- HY-120355A
-
|
Potassium Channel
|
Cardiovascular Disease
|
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
|
-
- HY-131032
-
|
Adenosine Receptor
|
Others
|
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively .
|
-
- HY-143312C
-
|
GLP Receptor
|
Metabolic Disease
|
(S)-V-0219 is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-143312E
-
|
GLP Receptor
|
Metabolic Disease
|
(S)-V-0219 hydrochloride is an enantiomer of V-0219 (HY-143312). V-0219 is an orally active and positive allosteric modulator (PAM) of the GLP Receptor-1 (GLP-1R). (S)-V-0219 hydrochloride activates calcium fluxes in HEK cells stably expressing hGLP-1R. (S)-V-0219 hydrochloride is orally active and ameliorates high glucose levels in mice and inhibits feeding behavior in fasted mice .
|
-
- HY-100588
-
|
mGluR
|
Neurological Disease
|
VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
|
-
- HY-100588A
-
|
mGluR
|
Neurological Disease
|
VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
|
-
- HY-136258
-
|
nAChR
|
Neurological Disease
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity .
|
-
- HY-133011
-
|
nAChR
|
Neurological Disease
|
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease .
|
-
- HY-130344
-
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression .
|
-
- HY-143880
-
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
|
-
- HY-156025
-
|
Others
|
Inflammation/Immunology
|
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis .
|
-
- HY-117467
-
|
Others
|
Neurological Disease
|
BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power. The effects of BMT-108908 differ from those of other NMDA receptor channel blockers such as ketamine and lanimol .
|
-
- HY-123525
-
|
Others
|
Neurological Disease
|
COR628 is a positive allosteric modulator of GABA(B) receptors with the activity of enhancing GABA-induced GTPγS stimulation. COR628 showed significant activity in in vitro studies but did not exhibit endogenous agonist activity. COR628 has shown efficacy in experiments in mice by enhancing the sedation/hypnosis induced by baclofen, shortening the onset time and extending the duration of loss of righting reflex when combined with non-sedating doses of baclofen . The cytotoxic effect of COR628 is comparable to or higher than that of GS39783 or BHF177 in concentration .
|
-
- HY-103412
-
|
Dopamine Receptor
Sigma Receptor
|
Neurological Disease
|
SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression .
|
-
- HY-116152
-
Ciprofol; HSK3486
|
GABA Receptor
Sirtuin
Keap1-Nrf2
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis .
|
-
- HY-118285
-
|
mGluR
|
Neurological Disease
|
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
|
-
- HY-111052
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
|
-
- HY-115860
-
|
Others
|
Neurological Disease
|
TAS-4 is a potent and selective mGluR4 positive allosteric modulator with significant anti-Parkinson's disease activity. TAS-4 is able to show efficacy when used alone or in combination with l-DOPA. TAS-4 is able to reverse haloperidol-induced spasticity when administered alone. TAS-4 enhances the contralateral rotation behavior induced by l-DOPA in a dose-dependent manner. TAS-4 combined with low-dose l-DOPA shows anti-Parkinson's effects similar to full-dose l-DOPA without exacerbating abnormal motor side effects .
|
-
- HY-136190
-
|
TRP Channel
|
Neurological Disease
|
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals .
|
-
- HY-103066
-
|
nAChR
|
Neurological Disease
|
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2,α2β4,α4β2,α4β4,(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit .
|
-
- HY-115857
-
|
Others
|
Neurological Disease
|
SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
|
-
- HY-131997
-
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response .
|
-
- HY-117106
-
|
GABA Receptor
|
Others
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PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
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- HY-120874
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GABA Receptor
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Neurological Disease
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PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
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HY-L170
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183 compounds
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An emerging drug design method is based on the secondary binding site effect, where small molecule drugs are designed to bind to secondary binding sites on target biomolecules rather than primary orthomorphic sites. Successful potential drugs (known as allosteric modulators) will be able to bind to allosteric sites and remotely alter (or modify) the conformation of the main orthosteric binding sites of biological targets. Allosteric modulators (AMs) are ligands of proteins that act through binding sites different from natural (orthosteric) ligand sites. AMs are relatively small, more lipophilic, and more rigid compounds. The binding efficacy of AMs with their targets is often slightly lower. AMs are divided into positive AMs (PAMs) and negative AMs (NAMs). AMs are ideal drug targets because they can fine-tune receptor activity while preserving the spatial and temporal signal transduction characteristics of endogenous ligands, resulting in fewer targeted side effects, improved subtype selectivity, and better promotion of biased signal transduction than normal ligands.
MCE designs a unique collection of 183 small allosteric modulators. It is a good tool to be used for research on metabolize, cancer and other diseases.
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Target |
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- HY-107663A
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Pro-Leu-Gly-NH2 TFA; Melanostatin TFA
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Dopamine Receptor
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Neurological Disease
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MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
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- HY-126327A
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Histone Methyltransferase
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Cancer
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UNC4976 TFA is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 TFA simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
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- HY-P1397A
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Cannabinoid Receptor
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Cardiovascular Disease
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RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also high affinity CB2 positive allosteric modulator (Ki=50 nM).
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- HY-P5860
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Micrurotoxin 1
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GABA Receptor
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Neurological Disease
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MmTx1 toxin (Micrurotoxin 1) is an allosteric GABAA receptor modulator that increases GABAA receptor susceptibility to agonist .
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- HY-107663
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Pro-Leu-Gly-NH2; Melanostatin
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Dopamine Receptor
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Neurological Disease
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MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .
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- HY-P1397
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Cannabinoid Receptor
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Neurological Disease
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RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2 .
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- HY-126327
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Histone Methyltransferase
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Cancer
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UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids. UNC4976 simultaneously antagonizes H3K27me3-specific recruitment of CBX7 to target genes while increasing non-specific binding to DNA and RNA .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99171
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Interleukin Related
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Inflammation/Immunology
Cancer
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Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
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Category |
Target |
Chemical Structure |
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Product Name |
Chemical Structure |
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Classification |
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- HY-118022
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Alkynes
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VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4?PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .
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