Table 3 GRK inhibitor profiling by 7TM phosphorylation assay.

From: A bead-based GPCR phosphorylation immunoassay for high-throughput ligand profiling and GRK inhibitor screening

 

GRK2/3 Inhibition Assay

GRK5/6 Inhibition Assay

Inhibitor

IC50 (µM)

IC50 (µM)

LDC9728

0.28 ± 0.03

0.08 ± 0.04

LDC8988

66.3 ± 1.29

0.33 ± 0.04

Compound101

2.87 ± 0.09

–

  1. Data represent the mean of n = 5 independent experiments performed in quadruplicates ± SE.
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