WEB2086
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Competition with [3H]PAF binding to human platelets: Ki = 9.9 nM |
| Selectivity within target family: > 30-fold | No close analogues known |
| Selectivity outside target family | Eurofins Safety screen (44 targets) at 10 µM [% Ctrl]: BZD/CENTR (rat) (12), PTGS2 (47); Benzodiazepine receptor inhibition (rat): Ki = 388 nM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Inhibition of PAF-induced human platelet aggregation: IC50 = 170 nM; Inhibition of PAF-induced human neutrophil aggregation: IC50 = 360 nM |
| Control compound (100 times less potent than the probe) | WEB2387: Human receptor binding Ki = 660 nM; Platelet aggregation IC50 = 8790 nMEurofins Safety screen (44 targets) at 10 µM: clean |