Potencies and efficacies of inverse agonists in the [35S]GTPγS binding assay
| Ligand | IC50 | % Binding over Control |
|---|---|---|
| nM | ||
| ICI-174864 | 176 ± 44 | 75 ± 2 |
| RTI-5989-1 | 13.6 ± 3.8 | 69 ± 3 |
| RTI-5989-23 | 8.2 ± 3.7 | 65 ± 2 |
| RTI-5989-25 | 6.6 ± 3.3 | 66 ± 4 |
Measurement of the ability of various ligands to inhibit [35S]GTPγS binding was performed as described underExperimental Procedures. Curves were fitted to a sigmoidal dose response curve with the Hill slope = −1 (GraphPad Prism; GraphPad, San Diego, CA). Values are the mean ± S.E.M. of three to five experiments.