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Competitive-inhibition experiments via fluorescence anisotropy of SB-284851-BT (I) and analogues against BET bromodomains indicating selectivity for BET D1s. (A) IC50 values of analogues (means ± SEM) determined by competitive-fluorescence-anisotropy assays. Asterisks (*) indicate incomplete inhibition observed; ND indicates not determined. (B) Competition-binding isotherms of compounds IV and V against the first and second bromodomains of BRD4 and BRDT.
