We have synthesized an extensive library of small molecule BET inhibitors with different chemical scaffolds and evaluated their pharmacological characteristics. These molecules have a range of different selectivity, potency, safety, and pharmacokinetic properties. For example, some compounds preferentially bind some BET family members (i.e. BRD4) over others, while others selectively target bromodomain 1 versus bromodomain 2 (BD1-selective vs. BD2-selective) on the same protein.
Recent studies have shown that targeting BD1 vs. BD2 domains result in inhibition of different sets of genes, and ultimately different biological outcomes. Our proprietary compound library allows us to select compounds with optimal sets of properties for each specific indication and combination.
