TABLE 3.
RGS4 cysteine mutant sensitivity to CCG-63802
Data are presented as mean ± S.E.M.
| RGS4 Mutant | IC50 | pIC50 Log(M) | Hill Slope | Inhibition at 100 μM | n |
|---|---|---|---|---|---|
| μM | % | ||||
| Wild type | 9 | 5.02 ± 0.07 | −0.86 ± 0.11 | 87 | 9 |
| C148A | 43 | 4.37 ± 0.07 | −0.95 ± 0.16 | 63 | 3 |
| C132A | 41 | 4.39 ± 0.07 | −0.97 ± 0.18 | 66 | 3 |
| C95A/C132A | 32 | 4.50 ± 0.13 | −0.78 ± 0.20 | 70 | 3 |
| C148A/C132A | 92 | 4.04 ± 0.07 | −0.75 ± 0.11 | 57 | 3 |
| C148A/C132A/C95A | ∼3000 | 2.55 ± 0.64 | −0.33 ± 0.12 | 16 | 3 |
| RGS4c | ∼8000 | 2.10 ± 1.50 | −0.36 ± 0.30 | 13 | 6 |
| A148C | ∼390 | 3.41 ± 0.17 | −0.62 ± 0.14 | 30 | 3 |
| A132C | 174 | 3.76 ± 0.19 | −0.80 ± 0.29 | 31 | 3 |
| A95C | 170 | 3.77 ± 0.23 | −1.20 ± 0.82 | 30 | 3 |
| A148C/A132C | 33 | 4.47 ± 0.05 | −1.48 ± 0.23 | 92 | 3 |
| A148C/A95C | 17 | 4.77 ± 0.12 | −1.06 ± 0.28 | 100 | 3 |
| A95C/A148C/A132C | 16 | 4.79 ± 0.12 | −0.63 ± 0.12 | 64 | 3 |