Search Result
Results for "
negative allosteric modulator
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114863
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THCCC
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mGluR
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Neurological Disease
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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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- HY-103561
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mGluR
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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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- HY-117959
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LPL Receptor
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Inflammation/Immunology
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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
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VU0483253
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mAChR
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Neurological Disease
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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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- HY-164764
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Estrogen Receptor/ERR
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Endocrinology
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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-119765
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-
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- HY-145585
-
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MIJ-821
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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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-
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- HY-103574
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ADX-10059 hydrochloride
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mGluR
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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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- HY-120527
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mGluR
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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-120428
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mGluR
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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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- HY-19630
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VU0463597
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mGluR
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Neurological Disease
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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-157998
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mGluR
Src
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Others
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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-16716
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RG1662; RO5186582
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GABA Receptor
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Neurological Disease
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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-116553
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Wnt
β-catenin
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Cancer
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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-129636A
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GABAB receptor antagonist 1
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GABA Receptor
ERK
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Neurological Disease
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(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-129636
-
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(E)-GABAB receptor antagonist 1
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GABA Receptor
ERK
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Neurological Disease
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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-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-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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- 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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- HY-124803
-
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GCGR
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Metabolic Disease
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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-145370
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iGluR
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Neurological Disease
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GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
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- HY-101845
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FITM
1 Publications Verification
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mGluR
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Cancer
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FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.
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- HY-112788
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-
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- HY-103573
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mGluR
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Neurological Disease
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VU 0360223 is a potent metabotropic glutamate receptors (mGluR) negative allosteric modulator with an IC50 of 61 nM .
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- HY-124393
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mGluR
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Neurological Disease
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GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
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- HY-16766
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RO4995819
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mGluR
|
Neurological Disease
|
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Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .
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- HY-119941
-
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mGluR
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Neurological Disease
|
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VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM .
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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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- HY-147657
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GABA Receptor
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Neurological Disease
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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 .
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- HY-122138
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mGluR
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Neurological Disease
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VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant .
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- HY-120375
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-
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- HY-114403
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mGluR
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Neurological Disease
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VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM .
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- HY-100667
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iGluR
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Neurological Disease
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UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .
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- HY-155088
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mGluR
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Metabolic Disease
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MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
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- HY-103491
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iGluR
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Neurological Disease
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PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates .
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- HY-129946
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- HY-133555
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mGluR
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Neurological Disease
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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 .
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- HY-168028
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mGluR
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Neurological Disease
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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 .
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- HY-124622
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GCGR
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Metabolic Disease
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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 .
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- HY-110278
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mGluR
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Neurological Disease
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ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .
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- HY-169345
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mGluR
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Neurological Disease
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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 .
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- HY-14866
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ADX-10059
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mGluR
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Neurological Disease
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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 .
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- HY-108710
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mGluR
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Neurological Disease
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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 .
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- HY-12629
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PF-06297470
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Others
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Others
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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.
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- HY-107774
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iGluR
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Neurological Disease
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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).
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- HY-101281
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mAChR
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Neurological Disease
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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 .
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- HY-135891
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CCR
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Neurological Disease
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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 .
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- HY-120699
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mGluR
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Neurological Disease
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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 .
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- HY-124569
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iGluR
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Neurological Disease
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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 .
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- HY-101281A
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mAChR
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Neurological Disease
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(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 .
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- HY-103572
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mGluR
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Neurological Disease
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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 .
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- HY-110180
-
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mGluR
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Neurological Disease
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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) .
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- HY-15446
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RG7090; CTEP Derivative
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mGluR
|
Neurological Disease
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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.
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- HY-155810
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iGluR
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Neurological Disease
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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 .
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- HY-107509
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mGluR
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Neurological Disease
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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 .
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- HY-103575A
-
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mGluR
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Neurological Disease
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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.
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- HY-120717
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mGluR
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Others
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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 .
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- HY-103575
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mGluR
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Neurological Disease
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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.
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- HY-19888
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P2X Receptor
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Inflammation/Immunology
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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 .
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- HY-103320A
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CaSR
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Metabolic Disease
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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) .
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- HY-131019
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mGluR
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Neurological Disease
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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 .
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- HY-103320
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CaSR
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Metabolic Disease
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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) .
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- HY-16636
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mGluR
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Neurological Disease
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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.
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- HY-14859
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ADX48621
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mGluR
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Neurological Disease
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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.
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- HY-129274
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mGluR
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Neurological Disease
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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-15469
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P2X Receptor
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Neurological Disease
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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 .
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- HY-15470
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P2X Receptor
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Neurological Disease
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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 .
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- HY-103118
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5-HT Receptor
Apoptosis
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Neurological Disease
Cancer
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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 .
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- HY-119282
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mGluR
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Neurological Disease
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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 .
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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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- HY-120355A
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Potassium Channel
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Cardiovascular Disease
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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) .
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- HY-117467
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Others
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Neurological Disease
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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 .
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- HY-118285
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mGluR
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Neurological Disease
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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.
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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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- 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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