1637770-13-8

GS-626510 is a potent BET family bromodomains inhibitor. It acts by targeting BRD2/3/4, and BRDT.

GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively[1].

BRD2: 0.59-2.5 nM (Kd); BRD3: 0.65-0.66 nM (Kd); BRD4: 1.3-3.2 nM (Kd); BD1: 83 nM (IC₅₀); BD2: 78 nM (IC₅₀)

[1] Sperandio D, et al. Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. DOI:10.1016/j.bmc.2018.11.020