TABLE 1

Kinase inhibitory activity of CCG258208 and CCG258747

Embedded Image
RCompoundGRK2 IC50 (μM)aGRK1 IC50 (μM)aGRK5 IC50 (μM)aPKA IC50 (μM)aROCK1b (%)
HParoxetine1.4 ± 1>100>100>10010
Embedded Image2582080.030 ± 0.00187 ± 307.1 ± 0.7>1009
Embedded Image2587470.018 ± 0.0069.3 ± 31.5 ± 0.5>10027
  • a All IC50 measurements are an average of three separate experiments run in duplicate. Errors shown represent error of the mean.

  • b Percent inhibition at 10 μM inhibitor concentration. IC50 data for paroxetine and CCG258208 are reproduced from Waldschmidt et al. (2017) for comparison.