-
Asenapine inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
More
-
Masitinib, a novel phenylaminothiazole-type derivative, is an inhibitor of the class III receptor tyrosine kinase stem-cell growth factor receptor (c-Kit) with IC50 of 200 nM, platelet-derived growth factor receptor α and β and the non-receptor tyrosine kinase Lyn(PDGFRα/β with IC50 of 540 nM/800 nM).
More
-
Quisinostat (JNJ-26481585) is a novel second-generation HDACi inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. , in NSCLC cells. In vitro, quisinostat has shown anti-proliferative activity against NSCLC cell lines. quisinostat extremely changed protein acetylation patterns of A549 cells and inhibited epithelial-mesenchymal transition (EMT) process.
More
-
Orteronel (TAK-700) is an inhibitor of the steroidogenic enzyme CYP17A1. It has higher specificity for the 17,20 lyase activity of CYP17A1 with IC50 of 38 nM. Phase III.
More
-
PBTZ169 is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.
More
