. Author manuscript; available in PMC: 2013 Nov 16.

Published in final edited form as: ACS Chem Biol. 2012 Aug 21;7(11):1830–1839. doi: 10.1021/cb3003013

Table 1.

Summary of ligand competition and Thermofluor data

	competition (2 nM C13.28-FAM)			ΔT_m (°C)

	pIC₅₀	n_H	n	GRK1	GRK2	GRK5
C13.28	9.3 ± 0.5	−0.9	4	N.D.	N.D.	N.D.
103A	8.6 ± 0.4	−0.8	6	6.2 ± 0.6^a	15.5 ± 0.7^a	3.6 ± 0.4^a
ATP	4.3 ± 0.3	−0.7	4	18.0 ± 1.5	4.9 ± 1.6	7.2 ± 1.1
sangivamycin	5.0 ± 0.3	−1.0	3	N.D.	N.D.	N.D.
P-835	5.5 ± 0.4	−1.6	4	−0.14 ± 0.1	1.2 ± 0.8	−0.007 ± 0.3
paroxetine	4.5 ± 0.2	−0.7	4	1.5 ± 1.1	7.8 ± 1.1	−0.4 ± 0.3

Values represent the mean ± SEM of n experiments, performed in duplicate (flow cytometry bead binding) or triplicate (Thermofluor). ΔT_m, change in melting temperature; n_H, Hill slope; N.D., not determined. With the exception of 103A, ligands in the Thermofluor assay were added to a final concentration of 200 μM.

Previously determined (23).