Synthesis and biological investigation of (+)-JD1, an organometallic BET bromodomain inhibitor

Synthesis and biological investigation of (+)-JD1, an organometallic BET bromodomain inhibitor

(+)-JD1, a rationally designed ferrocene analogue of the BET bromodomain (BRD) probe molecule (+)-JQ1, has been synthesized and evaluated in biophysical, cell-based assays as well as in pharmacokinetic studies. It displays nanomolar activity against BRD isoforms, and its cocrystal structure was dete...

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Bibliographic Details
Main Authors:	Hassell-Hart, S, Runcie, A, Krojer, T, Doyle, J, Lineham, E, Ocasio, CA, Neto, BAD, Fedorov, O, Marsh, G, Maple, H, Felix, R, Banks, R, Ciulli, A, Picaud, S, Filippakopoulos, P, von Delft, F, Brennan, P, Stewart, HJS, Chevassut, TJ, Walker, M, Austin, C, Morley, S, Spencer, J
Format:	Journal article
Published:	American Chemical Society 2019

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