JNJ-54082730
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: Scintillation proximity assay (SPA) for hPDE2A: IC50 = 0.9 (0.8 -1) nM, n= 93 [Mean (95% Confidence Interval)], Ki = 0.7 nM |
| Selectivity within target family: > 30-fold | Good CDK familiy selectivity: SPA (IC50 [nM]): hPDE10A2 (99), hPDE3 (6643); hPDE1B1, hPDE4D3, hPDE5A3, bovine retina PDE6, hPDE7A1, hPDE8A1, hPDE9A all IC50 > 10 µM |
| Selectivity outside target family | Eurofins Cerep panel: all IC50 > 10 µMDiscoverX KinaseScreen: > 1 µM, DCAMKL1 > 3 µM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Target occupancy Striatum ED50 = 5.3 mg/kg (p.o. 1 h, rat) |
| Control compound (100 times less potent than the probe) | JNJ-54103985: SPA for hPDE2A: IC50 = 97 nM, hPDE10A2 and hPDE3: IC50 > 10 µM; Target occupancy ED50 > 80 mg/kg (p.o. 1 h) |