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BI-1950

2D structure
Target ITGAL 
Targeted domain I-domain
Mode of action Inhibitor
Control BI-9446
Recommended cellular usage concentration 100 nM
In vivo use Yes
Donated by Boehringer Ingelheim


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) ITGAL binding assay: Kd = 9 nM
Selectivity within target family: > 30-fold Selective (>1000 fold) against closely related ITGB2 and ITGB1
Selectivity outside target family Cerep Panel available: at 10 µM; BI-1950 hit 4/47 off targets > 50 %, all four (CA+/DHPSI/RA, CA+/PAASITE, NA+/SITE2/RA and THRO SYN(HU)) : IC50 > 3 µM; Clean PDSP scan
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Inhibits staphylococcal enterotoxin B-induced production of IL2 in human PBMC (peripheral blood mononuclear cell), IC50 = 3 nM and whole blood, IC50 = 120 nM
Control compound (100 times less potent than the probe) Inhibits binding to ICAM1, Kd > 1000 nM; Inhibits SEB-induced production of IL2 in human PBMC, IC50 > 1000 nM; Clean PDSP scan except for activity on TMEM97 (Ki = 557.65 nM)