TABLE 1.
Interaction of small molecules with GRKs
Values represent mean ± S.E.M.
| GRK1 | GRK2 | GRK5 | GRK6 | |
|---|---|---|---|---|
| µM | ||||
| KD (paroxetine) | 13 | 7.3 | 14 | N.D. |
| Ki (paroxetine) (versus ATP) | 78 ± 10 | 3.5 ± 0.9 | N.D. | N.D. |
| KM (ATP) | 3.2 ± 0.5 | 8.8 ± 0.5 | N.D. | N.D. |
| KD (ADP) (FP) | 1.4 ± 0.2 | 46 ± 16 | N.D. | 11 ± 2 |
| KD (AMPPNP) (FP) | 49 ± 15 | 110 ± 20 | N.D. | 190 ± 7 |
| KD (balanol) (FP) | 0.55 ± 0.2 | 0.074 ± 0.07 | N.D. | 0.30 ± 0.15 |
| IC50 (balanol)a | 0.34 | 0.042 | 0.16 | 0.49 |
FP, measured by fluorescence polarization (this study); N.D., not determined.
a
From Tesmer et al., 2010.