PF-06649298 and PF-06761281 are potent inhibitors but low-affinity substrates
| EC50 agonist mode membrane potential (μM) | |||
|---|---|---|---|
| Citrate | Succinate | PF-06649298 | PF-06761281 |
| 216 ± 13 | 1018 ± 275 | N.D. | 4 ± 2 |
| IC50 antagonist mode membrane potential (μM) | |||
|---|---|---|---|
| Citrate | Succinate | PF-06649298 | PF-06761281 |
| N.D. | N.D. | 0.74 ± 0.23 | 0.36 ± 0.05 |
N.D., not determined. Data are averages ± S.E.M. from three independent experiments.