A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

B. Cox, Oakley; Krojer, T.; Collins, P.M.; Monteiro, Octovia; Talon, R.; Bradley, A.R.; Fedorov, O.; Amin, Jahangir; D. Marsden, Brian; Spencer, John; von Delft, F.; E. Brennan, Paul

doi:10.1039/c5sc03115j

Public

A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain

Published in Chemical Science • Dec 22, 2015

Authors:

Oakley B. Cox

T. Krojer

P.M. Collins

Abstract

values by an AlphaScreen competition assay. The follow-up libraries of four poised fragment hits improved potency into the sub-mM range while showing good ligand efficiency and detailed structural data.

Subject

Bromodomain

Fragment (logic)

Chemistry

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