JNJ-6204
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: CSNK1D: IC50 = 2.3 nM; CSNK1E: IC50 = 137 nM (purified Enzyme, ADP-GLO) |
| Selectivity within target family: > 30-fold | Closely related kinases: CSNK1A1 (IC50 = 419 nM)Panel of 370 kinases at 1 μM: clean; Closest hit: TNIK (IC50 = 1.6 μM) |
| Selectivity outside target family | Coming soon. |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion:CSNK1D: BRET whole cell binding assay: IC50 = 72 nM; PER2 translocation whole cell functional assay: IC50 = 542 nM |
| Control compound (100 times less potent than the probe) | JNJ-0293: Purified Enzyme, ADP-GLO: IC50 = 6.9 μM; BRET whole cell binding assay: IC50 > 10 μM |