Analysis of homologous competition-binding curves for CCK1R constructs
Values represent means ± S.E.M. of data from a minimum of three independent assays performed in duplicate. Two-tailed t tests were performed to determine the significance of differences.
| Constructs | T-0632 Binding | CCK Binding | ||
|---|---|---|---|---|
| Ki | Bmax | Ki | Bmax | |
| nM | (× 103/cell) | nM | (× 103/cell) | |
| WT | 2.3 ± 0.6 | 191 ± 55 | 3.6 ± 0.6 | 140 ± 36 |
| M121A | 42.4 ± 7.6* | 125 ± 40 | 13.2 ± 3.1 | 146 ± 39 |
| M195A | 3.0 ± 0.4 | 150 ± 46 | N.D. | N.D. |
| R197A | 3.0 ± 0.5 | 50 ± 21 | N.D. | N.D. |
| R197V | 2.5 ± 0.6 | 100 ± 35 | N.D. | N.D. |
| F198H/L199R | 1.8 ± 0.4 | 65 ± 17 | 3.5 ± 0.6 | 110 ± 34 |
| L200W | 0.4 ± 0.04* | 63 ± 20 | 1.5 ± 0.6 | 174 ± 40 |
| N202S | 2.6 ± 0.5 | 111 ± 39 | 8.3 ± 0.4* | 45 ± 15 |
| D203Ka | 0.9 ± 0.3 | 74 ± 13 | 3.1 ± 0.3 | 138 ± 10 |
| V204R | 3.2 ± 0.7 | 103 ± 44 | 3.3 ± 1.1 | 150 ± 39 |
| M205La | 1.4 ± 0.5 | 112 ± 21 | 2.1 ± 0.2 | 117 ± 30 |
| Q206R | 2.6 ± 0.6 | 146 ± 33 | 9.9 ± 0.9* | 145 ± 47 |
| S208T | 6.4 ± 1.2* | 170 ± 47 | 6.2 ± 2.0 | 145 ± 32 |
| W209A | N.D. | N.D. | N.D. | N.D. |
| R336Aa | N.D. | N.D. | N.D. | N.D. |