| DC11908 |
Ralaniten |
A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer. |
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| DC11909 |
Ralaniten acetate |
A novel small-molecule inhibitor of androgen receptor (AR) N-terminal domain inhibitor for the treatment of advanced prostate cancer. |
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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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| DC2710 |
Abiraterone (CB-7598) |
Abiraterone (CB-7598) is a potent CYP17 inhibitor with IC50 of 2 nM. |
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| DC7056 |
AMG-208
Featured
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AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM. |
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| DC10588 |
ASP-9521
Featured
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ASP-9521 is a potent, selective and orally available AKR1C3 inhibitor with an IC50 of 11 nM for human AKR1C3. |
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| DC7460 |
Masitinib
Featured
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Masitinib is a broad coronavirus 3CL inhibitor that effectively blocks replication of SARS-CoV-2. Science 20 Jul 2021: eabg5827 DOI: 10.1126/science.abg5827 |
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| DC5069 |
Enzalutamide (MDV3100)
Featured
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MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM. |
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| DC8700 |
ODM-201(Darolutamide)
Featured
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ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells. |
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| DC7160 |
SGI-1776
Featured
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SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. |
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| DC8008 |
TOK-001(Galeterone)
Featured
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TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC). |
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| DC9435 |
Zibotentan（ZD4054）
Featured
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Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM). |
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