Summary of AMG 580 properties
| Mol. Wt. = 473.51 | Potency to hPDE10A: IC50 = 0.13 nM | Selectivity over Other PDEs (PDE1–9, -11): IC50 > 30 μM |
|---|---|---|
| clogP = 2.62 | hP-gp Papp = 18; ER = 1 | rP-gp Papp = 16.8; ER = 1 |
| PSA = 101 | hFU = 0.006 | rFU = 0.007 |
| In vivo rat % ID/g = 1.2 | In vivo rat % ID/g = 1.2; in vivo rat AUC STR/THA = 23 | In vivo rat AUC STR/THA = 23 |
AUC, area under the curve; ER, efflux ratio; FU, unbound free fraction; h, human; ID, injected dose; Papp, apparent permeability coefficient; P-gp, P-glycoprotein; PSA, polar surface area; r, rat; STR, striatum; THA, thalamus.