| DC22277 |
A-420983
Featured
|
A-420983 is a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. |
|
| DC20611 |
A4250
Featured
|
A4250 (A-4250, Odevixibat) is a small molecule ileal bile acid transporter (IBAT) inhibitor for the treatment of cholestatic liver diseases including progressive familial intrahepatic cholestasis and NASH.. |
|
| DC8406 |
A-438079 HCl
Featured
|
A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
|
| DC7538 |
A66
Featured
|
A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms. |
|
| DC5163 |
A-674563
Featured
|
A-674563 is a potent, orally available Akt1 inhibitor with an IC50 value of 11nM. Also displays activity against PKA and CDK2 with IC50 values of 16nM and 46nM respectively. |
|
| DC7045 |
A-769662
Featured
|
A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity. |
|
| DC11372 |
A-779
Featured
|
A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay). |
|
| DC2061 |
A-803467
Featured
|
A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM. |
|
| DC9954 |
A 804598
Featured
|
A-804598 is a novel, competitive, and selective P2X7 receptor antagonist with IC50 of 10 nM, 9 nM and 11 nM in rat, mouse and human P2X7 receptors respectively. |
|
| DC7286 |
A83-01
Featured
|
A83-01 is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7 (IC50 values are 12, 45 and 7.5 nM respectively). |
|
| DC11304 |
A939572
Featured
|
A939572 is a potent, and orally bioavailable SCD1 inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively. |
|
| DC7046 |
A-966492
Featured
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively. |
|
| DC20616 |
AA 41612
Featured
|
AA 41612 is a potent, synthetic melanopsin antagonist with IC50 of 15.8 nM, attenuates melanopsin photocurrent in a dose-dependent manner. |
|
| DC23277 |
AA-115
Featured
|
AA-115 (APG 115) is a potent and orally active MDM2 inhibitor with Ki <1 nM, potently inhibits SJSA-1 cell growth with IC50 of 60 nM. |
|
| DC21979 |
ATF6 agonist compound A147
Featured
|
ATF6 agonist compound A147 is a specific, small molecule agonist of transcription factor ATF6, activates ATF6 and influences differentiation of stem cells.147 has broad antiviral activity against multiple DENV strains and serotypes and that the compound i |
|
| DC10165 |
AA26-9
Featured
|
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. |
|
| DC20618 |
AAI-101
Featured
|
AAI-101 is a novel extended-spectrum β-lactamase inhibitor with activity against many β-lactamases, including some class A and class D carbapenemases. |
|
| DC23864 |
AAL993
Featured
|
AAL993 (ZK260253) is a potent, orally active VEGFR inhibitor with IC50 of 130, 23 and 18 nM for VEGFR-1, 2 and 3, respectively. |
|
| DC10797 |
AB-423
Featured
|
AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies. |
|
| DC21981 |
CD73 inhibitor AB-680
Featured
|
AB680 (AB-680) is a highly potent, selective, reversible inhibitor of CD73 with Ki/IC50 of 4.9/70 pM (hCD73), displays > 10,000-fold selectivity against related ecto-nucleotidases (CD39, NTPDases 2/3/8) and a large panel of unrelated enzymes, receptors, a |
|
| DC8161 |
Xeglyze(Abametapir)
Featured
|
Abametapir is the active ingredient of Xeglyze Lotion. |
|
| DC11452 |
ABBV-744
Featured
|
ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy. |
|
| DC11299 |
ABC 1183
Featured
|
ABC1183 is a potent, selective, orally active GSK3α/β and CDK9 inhibitor with IC50 of 327/657 nM and 321 nM (CDK9/cyclin T1), shows growth inhibitory activity against a broad panel of cancer cell lines; decreases cell survival through G2/M arrest and modu |
|
| DC5027 |
ABC294640（Opaganib）
Featured
|
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. |
|
| DC24211 |
Abiraterone (D4A)
Featured
|
Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone. |
|
| DC20619 |
ABL127
Featured
|
ABL127 (ML174) is a potent, selective, covalent inhibitor of protein methylesterase 1 (PME-1) with IC50 of 10 nM. |
|
| DC8667 |
AB-MECA
Featured
|
AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors. |
|
| DC2002 |
Venetoclax(ABT-199)
Featured
|
Venetoclax (ABT-199; GDC-0199) is a highly selective, orally bioavailable small-molecule inhibitor of Bcl-2, exhibiting sub-nanomolar binding affinity with a Ki of less than 0.01 nM. This compound has been demonstrated to induce autophagy, highlighting its role in modulating programmed cell death pathways. In vitro studies reveal that Venetoclax exhibits potent cytotoxic activity against FL5.12-BCL-2 cells, with an EC50 of 4 nM, while showing markedly reduced efficacy against FL5.12-BCL-XL cells (EC50 = 261 nM), underscoring its selectivity for Bcl-2 over Bcl-XL.
The selectivity of Venetoclax is further corroborated in cellular mammalian two-hybrid assays, where it effectively disrupts BCL-2-BIM protein-protein interactions with an EC50 of 3 nM. In contrast, it demonstrates significantly weaker activity against BCL-XL-BCL-XS and MCL-1-NOXA complexes, with EC50 values of 2.2 μM, reinforcing its specificity for Bcl-2-dependent apoptotic regulation.
In vivo efficacy studies utilizing xenograft models derived from RS4;11 cells, a representative model of acute lymphoblastic leukemia (ALL), demonstrate that a single oral dose of Venetoclax (12.5 mg/kg) achieves a maximal tumor growth inhibition (TGImax) of 47% (P < 0.001) and a tumor growth delay (TGD) of 26% (P < 0.05). These results indicate robust anti-tumor activity in a Bcl-2-dependent malignancy. |
|
| DC4127 |
ABT-263 (Navitoclax)
Featured
|
ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively. |
|
| DC7352 |
ABT-333
Featured
|
ABT-333 is an NS5B non-nucleoside polymerase inhibitor. |
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