TABLE 3

RGS4 cysteine mutant sensitivity to CCG-63802

Data are presented as mean ± S.E.M.

RGS4 MutantIC50pIC50 Log(M)Hill SlopeInhibition at 100 μMn
μM%
Wild type95.02 ± 0.07−0.86 ± 0.11879
C148A434.37 ± 0.07−0.95 ± 0.16633
C132A414.39 ± 0.07−0.97 ± 0.18663
C95A/C132A324.50 ± 0.13−0.78 ± 0.20703
C148A/C132A924.04 ± 0.07−0.75 ± 0.11573
C148A/C132A/C95A∼30002.55 ± 0.64−0.33 ± 0.12163
RGS4c∼80002.10 ± 1.50−0.36 ± 0.30136
A148C∼3903.41 ± 0.17−0.62 ± 0.14303
A132C1743.76 ± 0.19−0.80 ± 0.29313
A95C1703.77 ± 0.23−1.20 ± 0.82303
A148C/A132C334.47 ± 0.05−1.48 ± 0.23923
A148C/A95C174.77 ± 0.12−1.06 ± 0.281003
A95C/A148C/A132C164.79 ± 0.12−0.63 ± 0.12643