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WEB2086

2D structure
Target PTAFR 
Mode of action Antagonist
Control WEB2387
Recommended cellular usage concentration 300 nM
In vivo use Yes
Synonyms Apafant, WEB 2086BS
Donated by Boehringer Ingelheim


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 nM
Eurofins Safety screen (44 targets) at 10 µM: clean