Affinities of three agonists for wild-type GRPR and NMBR and third extracellular GRPR point or group mutants.
| IC50 () | |||
|---|---|---|---|
| Bombesin | GRP | [d-Phe6, β-Ala11, Phe13, Nle14]Bn(6–14) | |
| nM | |||
| GRPR | 2.7 ± 0.2 | 2.7 ± 0.2 | 0.42 ± 0.04 |
| [D181E]GRPR | 2.7 ± 0.09 | 6.1 ± 0.2 | 0.50 ± 0.02 |
| [L182V]GRPR | 1.8 ± 0.09 | 5.7 ± 0.2 | 0.25 ± 0.02 |
| [H183A]GRPR | 1.6 ± 0.03 | 6.9 ± 0.4 | 0.60 ± 0.02 |
| [P184R]GRPR | 1.9 ± 0.07 | 5.9 ± 0.3 | 0.56 ± 0.04 |
| [F185I]GRPR | 71.8 ± 8.3 | 65.8 ± 7.6 | 0.75 ± 0.1 |
| [H186(–)]GRPR | 1.3 ± 0.02 | 6.4 ± 0.2 | 0.23 ± 0.02 |
| [VKDT187–190GSSD]GRPR | 2.8 ± 0.1 | ||
| [QT193,194SS]GRPR | 1.9 ± 0.06 | ||
| [IS195,196TA]GRPR | 1.0 ± 0.05 | 4.7 ± 0.3 | 0.68 ± 0.02 |
| [A198I]GRPR | 4.7 ± 0.4 | 42.8 ± 1.5 | 0.39 ± 0.02 |
| [HSN202–204QTD]GRPR | 1.6 ± 0.05 | 5.1 ± 0.1 | 0.43 ± 0.03 |
| [MA213,214VL]GRPR | 1.6 ± 0.1 | 6.3 ± 0.2 | 0.31 ± 0.04 |
| NMBR | 5.3 ± 0.4 | 30.8 ± 1.2 | 1.6 ± 0.1 |