TP-020
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: MGAT2 (human): IC50 = 7.8 nM; MGAT2 (mouse): IC50 = 2.4 nM (enzyme assay); |
| Selectivity within target family: > 30-fold | Surpasses criterion: >100-fold over mouse MGAT1 (IC50 = 2.6 µM), >1000-fold over human DGAT1 (IC50 > 30 µM), human DGAT2 (IC50 > 30 µM), human ACAT1 (IC50 = 19 µM) |
| Selectivity outside target family | Clean PDSP scan. |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | human MGAT1: IC50 = 160 nM (cell-based assay) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: IC50 = 3300 nM, more than 100-fold weaker than the probe candidate; Clean PDSP scan. |