Table 2 Mutant RGS4 Gαo binding affinities and 5nd logIC50s.
From: A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screen
Mutant | Gαo affinity (nM) | 5nd logIC50 (M) |
|---|---|---|
wild type | 11.6 ± 1.4 | -4.36 ± 0.03### |
C95A | 8.17 ± 1.5 | -4.71 ± 0.05### |
C148A | 6.84 ± 1 | -4.27 ± 0.05# |
C71A | 12.2 ± 1.8 | -4.34 ± 0.06## |
C132A | 7.9 ± 3.1 | -3.86 ± 0.07 |
-7C | 8.3 ± 1 | -3.24 ± 0.14*** |
A95C, -7C | 12 ± 2 | -3.58 ± 0.09** |
A148C, -7C | 5.7 ± 0.2 | -3.51 ± 0.09** |
A71C, -7C | 9.2 ± 2 | -3.20 ± 0.13** |
A132C, -7C | 12.5 ± 1 | -3.41 ± 0.09** |
no Cys in RGS domain | 3.9 ± 0.8 | -3.80 ± 0.06* |
no Cys in C-terminus | 5.0 ± 0.7 | -4.39 ± 0.07## |