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T8371 |
ML188
|
|
Virus Protease
,
SARS-CoV
|
|
ML188 is a selective noncovalent SARS-CoV 3CLpro inhibitor(IC50 : 1.5 μM), with moderate MW and good enzyme and antiviral inhibitory activity. |
|
T8926 |
Salcaprozate sodium
|
SNAC |
Others
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|
Salcaprozate sodium (SNAC), an oral absorption promoter, serves as a potent delivery agent for oral heparin and insulin by enhancing passive transcellular permeation through small intestinal epithelia. This is achieved t... |
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T10898 |
Samuraciclib hydrochloride
|
ICEC0942 hydrochloride,CT7001 hydrochloride |
Apoptosis
,
CDK
|
|
Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold h... |
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T11469 |
GSK-3484862
|
|
DNA Methyltransferase
|
|
GSK-3484862 is a non-covalent Dnmt1 inhibitor. It induces DNA hypomethylation to against cancer. |
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T9303 |
MRTX1133
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|
Ras
|
|
MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors. |
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T17389 |
AMAS
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Others
|
|
AMAS is a non-claevable heterobifunctional crosslinker with NHS ester and maleimide groups that enables covalent conjugation of amine- and sulfhydryl-containing molecules. |
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T8431 |
JCN037
|
|
EGFR
|
|
JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively). |
|
T11724 |
JNJ-42226314
|
|
Lipase
|
|
JNJ-42226314 is a highly selective non-covalent monoacylglycerol lipase (MAGL) inhibitor with anti-injury effects.JNJ-42226314 shows efficacy via endogenous cannabinoid-2-acryloylglycerol (2-AG) in models of neuropathic ... |
|
T40292 |
Opnurasib
|
NVP-JDQ443,JDQ-443,Opnurasib |
Ras
|
|
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer. |
|
T36287 |
Pirtobrutinib
|
|
BTK
|
|
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to t... |
|
T8766 |
GOT1 inhibitor-1
|
GOT1 inhibitor 2c |
Others
|
|
GOT1 inhibitor-1 (GOT1 inhibitor 2c) is a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. |
|
T9573 |
GSK3685032
|
|
DNA Methyltransferase
|
|
GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits c... |
|
T5461 |
GNE-6640
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|
DUB
|
|
GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23... |
|
T63098 |
SARS-CoV-2 Mpro-IN-2
|
|
|
|
SARS-CoV-2 MPro-IN-2 is a selective, low cytotoxic, non-covalent Mpro inhibitor with an IC50 value of 0.40 μM. SARS-CoV-2 Mpro-IN-2 showed good anti-SARS-CoV-2 effect with EC50 value of 1.1 μM. SARS-CoV-2 Mpro-IN-2 can b... |
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T40063 |
CBR-470-1
|
|
Nrf2
|
|
CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protect... |
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T72062 |
BI-2865
|
|
Ras
|
|
BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cel... |
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T38889 |
Thailanstatin A
|
|
|
|
Thailanstatin A is an ultra-potent inhibitor of eukaryotic RNA splicing (IC50 =650 nM). Thailanstatin A inhibits multiple cancer cell lines via non-covalent binding to the SF3b subunit of the U2 snRNA subcomplex of the s... |
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T10534 |
BI-4020
|
|
EGFR
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|
|
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T11159 |
EGFR-IN-2
|
|
EGFR
|
|
EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor. |
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T69545 |
Mpro 61
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|
|
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Mpro 61 is a potent non-covalent inhibitor of SARS-CoV-2 main protease. |
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T12621 |
(R)-FT671
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|
Others
|
|
(R)-FT671 is the R-isomer of FT671. FT671 is a potent, non-covalent and selective inhibitor of USP7 (IC50 of 52 nM) |
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T14915 |
CDK12-IN-E9
|
|
CDK
|
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM). |
|
T12621L |
FT671
|
|
DUB
|
|
|
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T10422 |
Avibactam free acid
|
NXL-104 free acid |
Antibacterial
|
|
Avibactam (NXL-104) free acid is a covalent and reversible inhibitor of non-β-lactam β-lactamase (IC50s: 8 nM and 5 nM for β-lactamase TEM-1 and CTX-M-15). |
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T19568 |
Sulfo-SMPB sodium
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|
Others
|
|
Sulfo-SMPB sodium is a non-cleavable heterobifunctional chemical cross-linking reagent that combines N-hydroxysuccinimide ester and maleimide groups. This compound enables the covalent conjugation of molecules possessing... |
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T63800 |
ZM223 hydrochloride
|
|
|
|
ZM223 hydrochloride is a potent, non-covalent, orally active inhibitor of NEDD8 activase (NAE). |
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T13412L |
ZM223 hydrochloride (2031177-48-5 free base)
|
ZM223 hydrochloride |
Serine Protease
|
|
ZM223 hydrochloride is an orally active, potent non-covalent inhibitor of NEDD8 activating enzyme (NAE), and with excellent anticancer activity. |
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T39859 |
ARN19689
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|
|
|
ARN19689 is an effective inhibitor of human NAAA, demonstrating high potency in the low nanomolar range (IC 50 = 0.042 μM). The compound acts through a non-covalent mechanism, highlighting its ability to interact with th... |
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T73510 |
ZG1077
|
|
|
|
ZG1077, a covalent KRAS G12C inhibitor, is utilized in non-small cell lung cancer (NSCLC) research. |
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T40358 |
Ensitrelvir fumarate
|
S-217622 fumarate |
|
|
Ensitrelvir (S-217622) fumarate is a novel orally active inhibitor, targeting the SARS-CoV-2 3CL protease (IC50 = 13 nM). It demonstrates non-covalent and non-peptidic characteristics. This compound represents a pioneeri... |
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T39648 |
(R)-GSK-3685032
|
|
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a first-in-class, non-time-dependent, non-covalent, reversible, selective DNMT1 inhibitor with an IC 50 of 0.036 μM. GSK-3685032 induces robust loss of D... |
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T35844 |
(R)-Pirtobrutinib
|
|
|
|
(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib, and Pirtobrutinib is a highly selective and non-covalent next generation BTK inhibitor. Pirtobrutinib (LOXO-305) effectively inhibits diverse... |
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T82137 |
IA1-8H2
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|
|
|
IA1-8H2, a non-covalent, non-competitive inhibitor of PHPT1 with an IC50 of 3.4 μM, is utilized in the study of lung cancer, hepatocarcinoma, and renal cancer [1]. |
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T26827 |
Bisnorcymserine
|
N1 N8 Bisnorcymserine,N1N8Bisnorcymserine,N1-N8-Bisnorcymserine |
|
|
Bisnorcymserine is a reversible inhibitor of butyrylcholinesterase. The leaving group, bisnoreseroline, interacts in a non-covalent way with Ser(200) and His(440), disrupting the existing interactions within the catalyti... |
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T75255L |
SB-435495 hydrochloride
|
|
|
|
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent, and orally active inhibitor of Lp-PLA2, exhibiting an IC50 of 0.06 nM [1] [3]. |
|
T39430 |
XMU-MP-3
|
|
|
|
XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-... |
|
T37085 |
Luxeptinib
|
|
|
|
Luxeptinib (CG-806) is a novel pan-FLT3/pan-BTK inhibitor that is administered orally. It exhibits potent and reversible inhibition of these enzymes, acting through a non-covalent mechanism. Luxeptinib effectively induce... |
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T75255L1 |
SB-435495 ditartrate
|
|
|
|
SB-435495 ditartrate is a potent, selective, reversible, non-covalent, and orally active inhibitor of Lp-PLA2, demonstrating an IC50 value of 0.06 nM [1] [3]. |
|
T79344 |
CDD-1819
|
|
SARS-CoV
|
|
CDD-1819, a non-covalent and non-peptide compound, serves as a potent SARS-CoV-2 Mpro inhibitor, exhibiting a K i value of 5 nM. It also effectively inhibits the Mpro variants ΔP168, A173V, and ΔP168/A173V [1]. |
|
T79346 |
CDD-1845
|
|
SARS-CoV
|
|
CDD-1845, a non-covalent, non-peptide inhibitor, exhibits potent inhibition of SARS-CoV-2 M^pro with a K_i value of 3 nM. Additionally, CDD-1845 is effective against M^pro variants ΔP168, A173V, and the combined ΔP168/A1... |
|
T79345 |
CDD-1733
|
|
SARS-CoV
|
|
CDD-1733 is a potent, non-covalent, and non-peptide inhibitor of the SARS-CoV-2 main protease (Mpro) with an inhibition constant (K i) of 12 nM. It effectively inhibits Mpro variants including ΔP168, A173V, and the combi... |
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T75109 |
HECT E3-IN-1
|
|
|
|
HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor that impedes Ub binding at the non-covalent Ub-binding site of Nedd4-1 [1]. |
|
T75255 |
SB-435495
|
|
|
|
SB-435495 is a compound characterized by its potent, selective, reversible, and non-covalent inhibition of Lp-PLA2, demonstrating an IC50 value of 0.06 nM. It is effective when administered orally. |
|
T9671 |
X77
|
|
|
|
X77 is an effective non-covalent inhibitor of the main protease of SARS-CoV-2 ( SARS-CoV-2 M pro ) [1]. X77 binds to SARS-CoV-2 M pro with a Kd value of 0.057 μM [2]. |
|
T74849 |
EBL-3183
|
|
|
|
EBL-3183, an indole-2-carboxylate, serves as a potent, reversible, non-covalent, and competitive inhibitor of metallo-β-lactamase (MBL), specifically targeting NDM-1 with a pIC50 of 7.7 [1]. |
|
T81849 |
MAT-POS-e194df51-1
|
|
SARS-CoV
|
|
MAT-POS-e194df51-1 is an orally active, non-covalent, non-peptide inhibitor of the SARS-CoV-2 main protease (M^pro) with an IC_50 of 37nM. It exhibits cytotoxicity, with EC_50 values of 64nM in A549-ACE2-TMPRSS2 cells an... |
|
T72762 |
Proteasome-IN-4
|
|
|
|
Proteasome-IN-4, a non-covalent proteasome inhibitor (IC 50 = 8.39 nM), exhibits potent antiproliferative effects on RPMI-8226, MM-1S, and MV-4-11 cell lines, making it valuable for cancer research. |
|
T63920 |
LSD1-IN-19
|
|
|
|
LSD1-IN-19 (compound 29) is a selective, potent, non-covalent inhibitor of LSD1 (Ki: 0.108 μM, KD: 0.068 μM). The 72h IC50 values were 0.17 and 0.40 μM, respectively. |
|
T79050 |
JBI-589
|
|
|
|
JBI-589 is an isoform-selective, non-covalent inhibitor of PAD4 that diminishes CXCR2 expression and impedes neutrophil chemotaxis. Additionally, it attenuates primary tumor growth and metastases, augmenting the efficacy... |
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T60874 |
Avibactam sodium dihydrate
|
|
|
|
Avibactam sodium (NXL-104) dihydrate inhibits CTX-M-15 and β-lactamase TEM-1 with IC 50 s of 5 nM and 8 nM, respectively. Avibactam sodium dihydrate is a reversible and covalent inhibitor of non-β-lactam β-lactamase [1]. |
