Search Result

Results for "

off-target

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (4) 5-HT Receptor (3) ADAMTS (1) ADC Linker (1) Amino Acid Decarboxylase (1) Apoptosis (4) Btk (2) Carbonic Anhydrase (2) Cathepsin (1) CDK (1) CRISPR/Cas9 (1) Dihydroorotate Dehydrogenase (1) DNA/RNA Synthesis (3) Dopamine Receptor (1) Drug Metabolite (1) Drug-Linker Conjugates for ADC (1) EGFR (2) Endogenous Metabolite (4) Epigenetic Reader Domain (3) ERK (2) Filovirus (1) Glutathione S-transferase (1) GSK-3 (1) Indoleamine 2,3-Dioxygenase (IDO) (1) Isotope-Labeled Compounds (1) Itk (1) Ligands for E3 Ligase (1) MAGL (2) Methionine Adenosyltransferase (MAT) (1) Microtubule/Tubulin (1) Molecular Glues (1) mTOR (1) Parasite (4) PKC (1) PROTACs (2) Radionuclide-Drug Conjugates (RDCs) (1) SARS-CoV (1) Sirtuin (1) Sodium Channel (1) TRP Channel (1) VEGFR (1) Virus Protease (1)
By Research Areas:	Cancer (23) Cardiovascular Disease (1) Infection (6) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (6)

By Targets:

5 alpha Reductase (4)

5-HT Receptor (3)

ADAMTS (1)

ADC Linker (1)

Amino Acid Decarboxylase (1)

Apoptosis (4)

Btk (2)

Carbonic Anhydrase (2)

Cathepsin (1)

CDK (1)

CRISPR/Cas9 (1)

Dihydroorotate Dehydrogenase (1)

DNA/RNA Synthesis (3)

Dopamine Receptor (1)

Drug Metabolite (1)

Drug-Linker Conjugates for ADC (1)

EGFR (2)

Endogenous Metabolite (4)

Epigenetic Reader Domain (3)

ERK (2)

Filovirus (1)

Glutathione S-transferase (1)

GSK-3 (1)

Indoleamine 2,3-Dioxygenase (IDO) (1)

Isotope-Labeled Compounds (1)

Itk (1)

Ligands for E3 Ligase (1)

MAGL (2)

Methionine Adenosyltransferase (MAT) (1)

Microtubule/Tubulin (1)

Molecular Glues (1)

mTOR (1)

Parasite (4)

PKC (1)

PROTACs (2)

Radionuclide-Drug Conjugates (RDCs) (1)

SARS-CoV (1)

Sirtuin (1)

Sodium Channel (1)

TRP Channel (1)

VEGFR (1)

Virus Protease (1)

By Research Areas:

Cancer (23)

Cardiovascular Disease (1)

Infection (6)

Inflammation/Immunology (3)

Metabolic Disease (2)

Neurological Disease (6)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Target Protein Ligand-Linker Conjugates Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114237

GDC-0276	Sodium Channel	Neurological Disease
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .

HY-124593

PTC299 2 Publications Verification	VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies .

HY-128027

eCF309	mTOR	Cancer
eCF309 is a potent and highly selective mTOR inhibitor with remarkably low off-target activities (IC₅₀ = 10-15 nM, both in vitro and in cells) .

HY-162941

SGD-9501-TFA	ADC Linker	Cancer
GD-9501-TFA is an auristatin S-based ADC linker with effective off-target toxicity characteristics, which can be used for the preparation of antibody-drug conjugates (ADCs) .

HY-145698

UCSF678	5-HT Receptor	Neurological Disease
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT_5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT_5AR .

HY-133084

ERK-IN-2	ERK	Cancer
ERK-IN-2 is a ERK2 inhibitor with an IC₅₀ value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM .

HY-133084A

ERK-IN-2 free base	ERK	Cancer
ERK-IN-2 free base is a ERK2 inhibitor with an IC₅₀ value of 1.8 nM. ERK-IN-2 free base might lead to off-target toxicity and/or off-target activity at dose >10 μM .

HY-145699

UCSF686	5-HT Receptor	Others
UCSF686 is a probe with which to study the function of the 5-HT_5AR. UCSF686 loses affinity at 5-HT_5AR (>10 000 nM) but not at 5-HT_1AR, 5-HT_2BR, and 5-HT₇R. UCSF686 controls for off-target effects .

HY-145951

Amidate-VC-PAB-MMAF	Drug-Linker Conjugates for ADC	Cancer
Amidate-VC-PAB-MMAF consists a cleavable ADC linker (Amidate-VC-PAB) and a potent tubulin polymerization inhibitor (MMAF). Amidate-VC-PAB-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs). Amidate-VC-PAB-MMAF reduces off-target cytotoxicity of ADCs .

HY-116793

Dimepiperate MY 93; Yukamate	MAGL	Others
Dimepiperate (MY 93) is a thiocarbamate (TC) pesticide. Dimepiperate has potential off-targets effect for the inhibition of ABHD6 .

HY-111094

NPD7155	Endogenous Metabolite	Cancer
NPD7155 is a purine-based competitive inhibitor of MTH1, designed to target cancer cells while exhibiting off-target effects that contribute to its cytotoxicity.

HY-13613

Dutasteride 3 Publications Verification GG 745; GI 198745	5 alpha Reductase Apoptosis	Cancer
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

HY-116793R

Dimepiperate (Standard)	MAGL	Others
Dimepiperate (Standard) is the analytical standard of Dimepiperate. This product is intended for research and analytical applications. Dimepiperate (MY 93) is a thiocarbamate (TC) pesticide. Dimepiperate has potential off-targets effect for the inhibition of ABHD6 .

HY-13056R

SMND-309 (Standard)	Drug Metabolite	Neurological Disease
Dimepiperate (Standard) is the analytical standard of Dimepiperate. This product is intended for research and analytical applications. Dimepiperate (MY 93) is a thiocarbamate (TC) pesticide. Dimepiperate has potential off-targets effect for the inhibition of ABHD6 .

HY-16984

GNE-4997	Itk	Inflammation/Immunology
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .

HY-13613R

Dutasteride (Standard) GG 745 (Standard); GI 198745 (Standard)	5 alpha Reductase Apoptosis	Cancer
Dutasteride (Standard) is the analytical standard of Dutasteride. This product is intended for research and analytical applications. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

HY-162284

BAY-9835	ADAMTS	Cardiovascular Disease
BAY-9835 is a potent and orally active ADAMTS7 and ADAMTS12 antagonist with IC₅₀s of 6 nM and 30 nM, respectively. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the atherogenesis research .

HY-13613S

Dutasteride-13C6 GG 745-¹³C₆; GI 198745-¹³C₆	Apoptosis 5 alpha Reductase	Cancer
Dutasteride- ¹³C₆ is the ¹³C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].

HY-125751

UCSF924	Dopamine Receptor	Neurological Disease
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC₅₀ of 4.2 nM. UCSF924 has no off-target effects on more than 320 non-olfactory GPCRs. UCSF924 can be used for research in the field of neuropsychiatric diseases .

HY-161956

Antiviral agent 59	Filovirus	Infection
Antiviral agent 59 (compound 58) is an antiviral agent with selective and drug-like properties that inhibits a broad spectrum of filoviruses. Antiviral agent 59 exhibits low off-target activity and inhibition against replication-competent Ebola virus (EBOV), Sudan virus (SUDV), and Marburg virus (MARV/b>) .

HY-E70219

SpCas9 D10A Nickase	CRISPR/Cas9	Others
SpCas9 D10A Nickase is a mutant of the Cas9 protein. SpCas9 D10A Nickase retains the function of a cleavage domain of Cas9 nuclease and specifically cleaves the target single strand to form a nick. SpCas9 D10A Nickase reduces off-target effects .

HY-126323

TCMDC-135051	Parasite	Infection
TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC₅₀=320 nM) .

HY-114939

Phelorphan	DNA/RNA Synthesis	Others
Phelorphan is a purine MTH1 inhibitor identified through chemical array screening. Although it targets cellular MTH1, its cytotoxicity to cancer cells is weaker than that of other reported inhibitors. The cytotoxicity of MTH1 inhibitors may be attributed to off-target effects, and MTH1 is not essential for cancer cell survival.

HY-126323B

TCMDC-135051 hydrochloride	Parasite	Infection
TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC₅₀=320 nM) .

HY-108331

3-TYP Maximum Cited Publications 69 Publications Verification	Sirtuin Methionine Adenosyltransferase (MAT) Indoleamine 2,3-Dioxygenase (IDO)	Cancer
3-TYP is an inhibitor of SIRT3 (IC₅₀of 38 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases .

HY-144793

Deac-SS-Biotin	Microtubule/Tubulin	Cancer
Deac-SS-Biotin is a potent antitumor agent with improved tumor targeting effects and reduced off-target toxicities. Deac-SS-Biotin uptakes into the cells through biotin-mediated internalization. Deac-SS-Biotin combined with DTT (Glutathione mimetic) can effectively inhibit microtubule assembly and displays greater antitumor activity .

HY-13613S2

Dutasteride-13C,15N,d GG 745-¹³C,¹⁵N,d; GI 198745-¹³C,¹⁵N,d	5 alpha Reductase Apoptosis Isotope-Labeled Compounds	Cancer
Dutasteride- ¹³C, ¹⁵N,d is ¹⁵N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

HY-122051

AC1903 1 Publications Verification	TRP Channel	Metabolic Disease
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .

HY-126323A

TCMDC-135051 TFA	Parasite	Infection
TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC₅₀=320 nM) .

HY-145226

XY-06-007	PROTACs Epigenetic Reader Domain	Cancer
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4_BD1L94V degrader. XY-06-007 shows a DC_{50, 6 h} of 10 nM against BRD4_BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies .

HY-155534

17β-HSD10-IN-1	Endogenous Metabolite	Others
17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability. 17β-HSD10-IN-1 doesn't result additional effects for mitochondrial off-targets and cytotoxic or neurotoxic effects .

HY-19985A

(3S,4S)-PF-06459988	EGFR	Cancer
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .

HY-115822

α-Fluoromethylhistidine dihydrochloride	Amino Acid Decarboxylase Glutathione S-transferase	Metabolic Disease
α-Fluoromethylhistidine dihydrochloride is a potent irreversible inhibitor of histidine decarboxylase (HDC) and glutathione S-transferase, demonstrating significant potential in studying histidine metabolism and drug metabolism processes. α-Fluoromethylhistidine dihydrochloride offers an effective approach to inhibit enzymes involved in these metabolic pathways. α-Fluoromethylhistidine dihydrochloride has implications for drug development by revealing off-target effects that may influence physiological drug metabolism and elimination mechanisms.

HY-161596

SmCB1-IN-1	Parasite Cathepsin	Infection
SmCB1-IN-1 (Compound 2h) is an inhibitor for S. mansoni cathepsin B1 (SmCB1) with an K_i of 0.05 μM . SmCB1-IN-1 exhibits selectivity toward human off-target cathepsins (29% and 37% inhibition for CatB and CatL at 20 μM). SmCB1-IN-1 inhibits 68% Schistosoma mansoni at 1 μM .

HY-156181

hCAIX/XII-IN-8	Carbonic Anhydrase	Cancer
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with K_i values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .

HY-131328

Pirtobrutinib 3 Publications Verification LOXO-305	Btk	Cancer
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM .

HY-137464A

OATD-01 1 Publications Verification	Others	Inflammation/Immunology
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC₅₀=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .

HY-156654

Ibuzatrelvir PF-07817883	SARS-CoV Virus Protease	Infection
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M ^pro and 3CL ^pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .

HY-155535

17β-HSD10-IN-2	Endogenous Metabolite	Neurological Disease
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .

HY-150279

PolQi2 1 Publications Verification	DNA/RNA Synthesis	Others
PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9, significantly improving the fidelity and performance of CRISPR/Cas9 gene editing. PolQi2 can be used in gene editing research .

HY-148561

CDK8-IN-12	CDK GSK-3 PKC	Cancer
CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a K_i of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with K_is of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent .

HY-P10761

DPI-4452	Radionuclide-Drug Conjugates (RDCs) Carbonic Anhydrase	Cancer
DPI-4452 is a *CAIX*-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC₅₀ for recombinant hCAIX: 130?nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

HY-155072

PROTAC BTK Degrader-5	PROTACs Btk	Cancer
PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC₅₀ value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898)) ¹.

HY-116163

ML350 CYM50202	Endogenous Metabolite	Others
ML350 (CYM50202) is a highly potent OPRK1 antagonist with selectivity and broad biological applications. With IC₅₀ values of 9-16 nM, ML350 shows high selectivity for OPRK1, with selectivity of 219-382-fold and 20-35-fold relative to OPRD1 and OPRM1, respectively. ML350 exhibited favorable characteristics in in vivo pharmacokinetic analysis, including high passive membrane permeability and moderate human plasma protein binding. Extensive screening of ML350 against multiple ion channels, receptors, and transporters showed that it does not have adverse off-target effects .

HY-147319

RTI-7470-44	Others	Neurological Disease
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .

HY-160695

PT-179	Ligands for E3 Ligase Molecular Glues	Cancer
PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms .

HY-P2548

pp60 (v-SRC) Autophosphorylation Site, Phosphorylated	EGFR	Others
pp60 (v-SRC) Autophosphorylation Site, Phosphorylated is the phosphorylated peptide of an EGFR substrate. pp60 (v-SRC) Autophosphorylation Site, Phosphorylated can be used for the screening of EGFR Kinase inhibitors via phosphorylated-substrate quantification .

HY-114205A

TP-238 hydrochloride	Epigenetic Reader Domain	Cancer
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC₅₀ values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC₅₀ of 5.9 and is less active against other 338 kinases .

HY-114205

TP-238	Epigenetic Reader Domain	Cancer
TP-238 is a potent and selective dual CECR2/BPTF probe with IC₅₀ values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC₅₀ of 5.9 and is less active against other 338 kinases .

HY-16729A

Relenopride hydrochloride YKP10811 hydrochloride	5-HT Receptor	Inflammation/Immunology
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT₄ receptor agonist (K_i=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT_2A (K_i=600 nM) and 5-HT_2B receptors (K_i=31 nM) than for 5-HT₄. Relenopride hydrochloride increases gastrointestinal (GI) motility .

Cat. No.	Product Name

HY-L036

Covalent Screening Library

1,450 compounds

Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.

MCE covalent inhibitor library contains 1,450 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

HY-L908

Lead-like Covalent Screening Library

1,049 compounds

MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.

HY-L036P

Covalent Screening Library Plus

5,738 compounds

MCE covalent inhibitor library contains 5,738 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.

MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.

Cat. No.	Product Name	Target	Research Area