79425-89-1Relevant articles and documents
INHIBITORS OF RPN11
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, (2017/03/14)
Candidate compounds for specific inhibition of Rpn11 are represented by Formula 1a where each of R2, R3, R4, R5, R6, and R7 is independently selected from hydrogen (H), substituted and unsubstituted alkyl groups, carboxyl groups, or substituted and unsubstituted carboxyamides.
Discovery of potent and orally bioavailable inhibitors of Human Uric Acid Transporter 1 (hURAT1) and binding mode prediction using homology model
Peng, Jianbiao,Hu, Qiyue,Gu, Chunyan,Liu, Bonian,Jin, Fangfang,Yuan, Jijun,Feng, Jun,Zhang, Lei,Lan, Jiong,Dong, Qing,Cao, Guoqing
supporting information, p. 277 - 282 (2016/01/09)
This Letter describes the discovery of a series of potent inhibitors of Human Uric Acid Transporter 1 (hURAT1). Lead generation and optimization via 3D pharmacophore analysis resulted in compound 41. With an IC50 of 33.7 nM, 41 also demonstrated good oral bioavailability in rat (74.8%) and displayed a consistent PK profile across all species tested (rat, dog and monkey).