TABLE 2

Kinase activity of alkylated indazole-paroxetine hybrids

CCG#	R	GRK2 IC₅₀ (μM)^{^a}	GRK1 IC₅₀ (μM)^{^a}	GRK5 IC₅₀ (μM)^{^a}	PKA IC₅₀ (μM)^{^a}	ROCK1^{^b} (%)
224061	H	0.066 (1.1)	6.4 (1.3)	1.3 (1.2)	3.1 (1.4)	100 ± 1.5
258001	Me	0.28 (1.5)	52 (1.1)	33 (1.2)	85 (1.2)	61 ± 5.3
258211	Et	0.96 (1.3)	>100	>100	>100	45 ± 1.5
258746	iPr	1.8 (1.2)	>100	>100	NT	33 ± 10.3

↵^a All IC₅₀ measurements are reported as the geometric mean of three separate experiments run in duplicate. Error is expressed in parenthesis as the geometric S.D. factor (multiplied or divided by the mean).
↵^b Percent inhibition at an inhibitor concentration of 10 μM, error is expressed as the S.D.