TABLE 1

Interaction of small molecules with GRKs

Values represent mean ± S.E.M.

GRK1GRK2GRK5GRK6
µM
KD (paroxetine)137.314N.D.
Ki (paroxetine) (versus ATP)78 ± 103.5 ± 0.9N.D.N.D.
KM (ATP)3.2 ± 0.58.8 ± 0.5N.D.N.D.
KD (ADP) (FP)1.4 ± 0.246 ± 16N.D.11 ± 2
KD (AMPPNP) (FP)49 ± 15110 ± 20N.D.190 ± 7
KD (balanol) (FP)0.55 ± 0.20.074 ± 0.07N.D.0.30 ± 0.15
IC50 (balanol)a0.340.0420.160.49
  • FP, measured by fluorescence polarization (this study); N.D., not determined.

  • a From Tesmer et al., 2010.