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Description

A selective inhibitor of beta-adrenergic receptor kinase 1 (betaARK1) (IC50 = 126 µ,M). Displays no inhibitory activity against protein kinase A (PKA). Identified from a group of existing compounds (not previously demonstrated to inhibit betaARK1) using a two-step rational drug design protocol that included molecular modeling and comparative docking studies. Represents the first inhibitor that distinguishes between betaARK1 and PKA, an enzyme with a similar adenine binding pocket. May be useful in the study of mechanisms involved in congestive heart failure where elevated levels of betaARK1 desensitize agonist-bound beta2-adrenergic receptors., A selective inhibitor of betaARK1 (beta-Adrenergic Receptor Kinase 1) (IC50 = 126 µ,M). Has no inhibitory activity against protein kinase A (PKA).