Table 2. In vitro Radioligand Competition Binding Assay.
| +NBI-42902 | ||||
| pIC50 (nM) | Bmax | pIC50 (nM) | Bmax | |
| Wild type | 8.54±0.04 (2.88) | 100±2 | 8.56±0.17 (2.75) | 93±13 |
| Glu90Lys | nb | nb | 8.21±0.06 (6.17) | 134±8* |
| Pro282Arg | nb | nb | nb | nb |
| Tyr323Cys | 8.85±0.11 (1.41) | 45±5 | 8.90±0.10 (1.26) | 71±6* |
Ligand binding affinity (pIC50) were measured on intact COS-7 cells transfected with wild type and mutant receptors by competition binding using 125I-His5-D-Tyr6-GnRH1.
B max = % of total radioligand bound were expressed relative to wild type receptor without NBI-42902.
nb
No measurable binding.
Values are mean ± SEM of three or more independent experiments, converted to nM (in parentheses).
Significant difference of NBI-42902 treatment on B max is represented by an asterisk * (p<0.05).