THPP-1
| Target | PDE10A |
| Targeted domain | Active site |
| Mode of action | Inhibitor |
| Control | THPP-1-NC |
| Orthogonal probe | JNJ-42396302 |
| Recommended cellular usage concentration | 100 nM |
| In vivo use | Yes |
| Donated by | MSD |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: PDE10A: Ki = 0.99 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: PDE selectivity: closest hit is PDE6A (44x) |
| Selectivity outside target family | Screened at Panlabs @ 10 µM; closest off off-target: Adenosine transporter (guinea pig): IC50 = 1.61 µMClean PDSP scan except for weak activity on TMEM97 (Ki = 3350.43 nM)KINOMEScan with 468 targets atv100 nM: Closest off-target of primary data (% Ctrl) is AKT3 (47) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses: Cell assay IC50 = 49 nM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: PDE10A potency 500x less (Ki = 522 nM). Clean PDSP scan except for activity on HTR7 (Ki = 577.7 nM) and TMEM97 (Ki = 707.78 nM)KINOMEScan with 468 targets at 100 nM: clean |