TP-024
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: CHO-based cAMP assay, EC50: 93 nM (human), 141 nM (mouse), 134 nM (rat) |
| Selectivity within target family: > 30-fold | GPR52 belongs to cluster1 class A GPCR family that also includes GPR21. However selectivity over them are not examined. Clean PDSP scan. |
| Selectivity outside target family | No significant activity at 10 μM. That means more than >100 selectivity (Ricerca) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: CHO-based cAMP assay, EC50 : 93 nM (human), 141 nM (mouse), 134 nM (rat) |
| Control compound (100 times less potent than the probe) | human GPR52: EC50 >1000 nM (cell assay); EC50 TP-024/TP-024n ≥ 100-fold; Clean PDSP scan |