Table 1. Functional properties of partial agonists and AgoPAMs in human, rat, and mouse GPR40 IP accumulation assays.
| Potency [EC50, nM] ± SD and Efficacy (% Activation) | |||
|---|---|---|---|
| Human | Rat | Mouse | |
| AP1 | 0.15 ± 0.05 | 0.59 ± 0.28 | 0.51 ± 0.12 |
| (359%) | (531%) | (532%) | |
| AP3 | 0.48 ± 0.25 | 1.3 ± 0.63 | 1.2 ± 0.72 |
| (318%) | (405%) | (478%) | |
| MK-2305 | 24 ± 13 | 5.2 ± 2.5 | 2.6 ± 0.8 |
| (85%) | (155%) | (157%) | |
| MK-8666 | 0.54 ± 0.22 | 1.6 ± 0.69 | 0.89 ± 0.41 |
| (86%) | (149%) | (143%) | |
| TAK-875 | 4.0 ± 2.2 | 7.8 ± 4.0 | 4.4 ± 2.1 |
| (102%) | (158%) | (145%) | |
| AMG-837 | 2.2 ± 0.6 | 1.5 ± 0.41 | 1.9 ± 0.76 |
| (78%) | (173%) | (149%) | |
| AM-1638 | 3.7 ± 1.9 | 41 ± 21 | 36 ± 11 |
| (200%) | (373%) | (402%) | |