EUB0000195c_EP300@BRD

Screened at 2 µM via biolayer interferometry (BLI), weak inhibition of BET bromodomains at 2.0 µM (BRD2, BRD3, BRD4, BRDT on both BD1 and BD2), clean at screen with 200 nM; DSF assay screen against 43 bromodomain family members, closest targets: dTM(BRD2, BD1) = 1.35 K, dTM(BRD3, BD1) = 1.55 K, dTM(BRD4, BD1) = 2.09 K, dTm(BRD4, BD2) = 0.58 K; In vitro follow-up (ITC): Kd(BRD4, BD1) = 5.6 µM, Kd(BRD4, BD2) = 20 µM; Screened in CEREP selectivity panel against 104 targets (nuclear receptors, ion channels, and 32 enzyme assays (including 10 kinases, 9 proteases, and 5 phosphodiesterases) at 10 µM, closest targets as % of inhibition: a1A (89%), M2 (67%);