TABLE 1.
Ki values (in nm) of compounds from different pharmacological classes determined from competition binding fluorescent assays between JMV 4946 and the different monomeric and dimeric purified receptors
| Ghrelin | MK 0677 | JMV 3002 | JMV 3011 | SPA | |
|---|---|---|---|---|---|
| GHS-R1a | 78.4 ± 8.2 | 65.8 ± 6.3 | 9.2 ± 2.7 | 8.3 ± 3.3 | 293.7 ± 10.2 |
| GHS-R1b | |||||
| GHS-R1aE124Q | 912 | 993 | 915 | 852 | |
| GHS-R1a:GHS-R1a | 75.6 ± 7.7 | 68.4 ± 7.2 | 9.9 ± 2.5 | 10.2 ± 3.9 | 286.3 ± 12.8 |
| GHS-R1a:GHS-R1b | 109.6 ± 6.2 | 90.6 ± 5.3 | 19.3 ± 3.3 | 9.9 ± 2.8 | 291.8 ± 9.2 |
| GHS-R1a:GHS-R1aE124Q | 79.4 ± 5.6 | 68.9 ± 2.3 | 8.7 ± 3.8 | 8.9 ± 4.2 | 299.6 ± 6.5/988 |