MRL-SYKi
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | Human SYK enzyme IC50: 0.9±0.4 nM |
| Selectivity within target family: > 30-fold | Surpasses criterion: Profiled in an Invitrogen panel of 265 kinases: > 100-fold kinome selective, 28 kinases fell within the 100-1000-fold selectivity window. The closest off-target kinases were SRC (IC50 = 100 nM), NTRK1 28 (IC50 = 105 nM) and NTRK3 (IC50 = 120 nM). |
| Selectivity outside target family | Profiled in a panel of 113 enzymes and receptors at MDS Pharma/Taiwan at 10 µM: clean; Clean PDSP scan |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: < 100 nM in a cellular assay and < 300 nM in human whole blood |
| Control compound (100 times less potent than the probe) | Surpasses criterion: The negative control is 1000-fold less potent biochemically and shows no activity in cells @ 10µM; Note: Shows off-target activity in the PDSP scan: the closest hit is GABA/PBR (Ki = 774 nM) |