UCSF924
Probe criteria
| Selectivity within target family: > 30-fold | Surpasses criterion:Tested D2-like family (DRD2 Ki > 10 µM , DRD3 Ki > 10 µM) > 3300-fold selectivity; No activity in panel of 320 non-olfactory GPCRs at 1 µM.Closest hits in the PDSP scan are HTR1A (Ki =223.0 nM), HTR2B (Ki =236.67 nM), HTR7 (Ki =2075.67 nM). |
| Selectivity outside target family | Not tested |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion:EC50 of 4.2 nM in cAMP receptor assay; EC50 of 0.2 nM in BRET-Gi dissociation assay |
| On target cell activity for secreted targets: | In vivo: Following a single i.p. administration of UCSF924 to male C57BL/6 mice at 10 mg/kg dose, plasma concentrations were quantifiable up to 12 hr with Tmax at 0.5 hr. Brain concentrations of UCSF924 were quantifiable up to 8 hr. |
| Control compound (100 times less potent than the probe) | Surpasses criterion:In vitro: Ki = 7500 nM; 2500 times less potent than the probe; Cell activity: EC50 not detectable (cAMP reporter assay) |
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | Surpasses criterion:DRD4: Ki = 3 nM, EC50 = 4.2 nM |