TP-021
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: BCL6: IC50 = 100 nM (ELISA) |
| Selectivity within target family: > 30-fold | Compound is PPI (Protein Protein Inhibition) inhibitor targetting non-conserved sites |
| Selectivity outside target family | TP-021 and TP-021n show no significant inhibition at 1 μM in Takeda in house kinase panel (344 targets); Clean PDSP scan |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: IC50 = 0.72 μM cell-based mammalian two-hybrid assay (M2H) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: IC50 = 110 μM (ELISA), more than 1,000-fold weaker than the probe candidate; Clean PDSP scan |