KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16?μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases. 了解更多
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. 了解更多
GeA-69 is a selective, highly cell permeable allosteric inhibitor of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) targeting macrodomain 2, with a Kd of 2.1 ?M. 了解更多
DS-1040 Tosylate is an inhibitor of the activated thrombin-activatable fibrinolysis inhibitor (TAFIa), used for the treatment of acute ischemic stroke (AIS). 了解更多
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively. 了解更多
(S,R,S)-AHPC TFA (MDK7526 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA (MDK7526 TFA) can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells. 了解更多
Anti-Heart Failure Agent 1 an orally available compound suitable for the treatment of heart failure without inducing nausea, vomiting and restlessness. 了解更多
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a. 了解更多
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile. 了解更多
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC). 了解更多
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM. 了解更多
Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. 了解更多
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level. 了解更多
Brian F Kiesel, .et al. Dose-dependent bioavailability, absorption-rate limited elimination, and tissue distribution of the ATR inhibitor BAY-1895344 (elimusertib) in mice, Cancer Chemother Pharmacol, 2022, Jun;89(6):795-807 PMID: 35507041
ligand for the α2δ subunit of voltage-gated calcium channels
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. 了解更多
AcLys-PABC-VC-Aur0101 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0101 (an auristatin microtubule inhibitor), linked via the cleavable linker AcLys-PABC-VC. 了解更多
AmPEG6C2-Aur0131 is a drug-linker conjugate for ADC (anti-CXCR4 ADC) with potent antitumor activity by using Aur0131 (an auristatin microtubule inhibitor), linked via the non-cleavable linker AmPEG6C2. 了解更多
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor. 了解更多
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity. 了解更多
PI3Kγ inhibitor 3 is a potent and remarkably selective PI3Kγ inhibitor with pIC50s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively. 了解更多
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the Modified MMAF (a tubulin inhibitor), linked via the noncleavable MC-Alkyl-Hydrazine. 了解更多
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain. 了解更多
PEG4-aminooxy-MMAF is a drug-linker conjugate for ADC with potent antitumor activity by using the potent antitubulin agent MMAF, linked via the noncleavable PEG4. 了解更多
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