DC21981 |
CD73 inhibitor AB-680
Featured
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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 |
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DC9029 |
Abacavir |
Abacavir is a powerful nucleoside analog reverse transcriptase inhibitor (NRTI) used to treat HIV and AIDS. |
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DC8161 |
Xeglyze(Abametapir)
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Abametapir is the active ingredient of Xeglyze Lotion. |
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DC11452 |
ABBV-744
Featured
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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. |
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DC11299 |
ABC 1183
Featured
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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 |
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DC5027 |
ABC294640(Opaganib)
Featured
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ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. |
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DC10929 |
ABC99 |
ABC99 is a potent, selective inhibitor of the Wnt-deacylating enzyme serine hydrolase NOTUM with IC50 of 13 nM, shows excellent selectivity across the serine hydrolase family. |
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DC12444 |
ABD-1970 |
ABD-1970 (ABD1970) is a highly potent, selective Monoacylglycerol lipase (MGLL) inhibitor with IC50 of 13 nM (human MGLL). |
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DC11925 |
ABD328 |
ABD328 (ABD-328) is an orally active, small molecule inhibitor of RANKL and TNF signalling that inhibits inflammation in vivo. |
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DC20620 |
ABD345 |
ABD345 is a small molecule inhibitor of RANKL signalling, inhibits TNF-induced NF-κB and MAPK activation and inflammation. |
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DC23586 |
Abeprazan |
Abeprazan is an acid pump inhibitor.. |
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DC2710 |
Abiraterone (CB-7598) |
Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM. |
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DC24211 |
Abiraterone (D4A)
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Abiraterone (D4A) is an active metabolite of the CYP17A1 inhibitor abiraterone. |
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DC20619 |
ABL127
Featured
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ABL127 (ML174) is a potent, selective, covalent inhibitor of protein methylesterase 1 (PME-1) with IC50 of 10 nM. |
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DC20298 |
ABL-IN-29 |
ABL-IN-29 is a picomolar ABL kinase inhibitor with IC50 of 0.06/0.11 nM for wt ABL and ABL T315I respectively.. |
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DC20299 |
ABMA |
ABMA is a novel broad-spectrum inhibitor of intracellular toxins and pathogens, efficiently protects cells against various toxins and pathogens including viruses, intracellular bacteria and parasite. |
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DC8667 |
AB-MECA
Featured
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AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors. |
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DC21983 |
Abn-CBD |
Abn-CBD (Abnormal Cannabidiol) is a selective agonist of GPR55 receptor with EC50 of 2.5 uM, shows no significant activity against CB1 and CB2 receptors (EC50>30 uM). |
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DC11762 |
ABP-A3 |
ABP-A3(ABP A3) is an inhibitor of ubiquitin conjugation that targets ubiquitin and Nedd8 E1 enzymes. |
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DC20625 |
ABT-072 |
ABT-072 is a novel, orally bioavailable non-nucleoside HCV NS5B polymerase inhibitor with EC50 of 0.3 nM (GT1b). |
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DC22258 |
ABT-080 |
ABT-080 is a potent FLAP inhibitor that inhibits ionophore-stimulated LTB(4) formation with with IC50 of 20 nM. |
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DC20626 |
ABT-089 |
ABT-089 (Pozanicline) is a potent, selective α4β2 nAChR agonist with Ki of 16 nM. |
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DC21984 |
ABT-100 |
ABT-100 (ABT100) is a highly selective, potent, orally bioavailable inhibitor of farnesyltransferase (FTase). |
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DC20628 |
ABT-102 |
ABT-102 is a potent, highly selective, orally active TRPV1 antagonist that inhibits agonist-evoked increases in intracellular Ca(2+) levels with IC50 of 5-7 nM. |
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DC20629 |
ABT-107 |
ABT-107 is a potent and selective α7 nAChR agonist with Ki of 0.2-0.6 nM for rat or human cortex α7 nAChRs. |
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DC2002 |
Venetoclax(ABT-199)
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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. |
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DC4127 |
ABT-263 (Navitoclax)
Featured
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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. |
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DC23537 |
ABT-288 |
ABT-288 is a potent, selective and competitive antagonist of H3 receptor with Ki of 1.9/8.2 nM for human/rat H3 respectively. |
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DC7352 |
ABT-333
Featured
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ABT-333 is an NS5B non-nucleoside polymerase inhibitor. |
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DC10049 |
Tebanicline(ABT-594)
Featured
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ABT-594 represents a novel class of broad-spectrum analgesics whose primary mechanism of action is activation of the neuronal nicotinic acetylcholine receptors. |
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