BI 665915
| Target | ALOX5AP |
| Targeted domain | Membrane domain |
| Mode of action | Inhibitor |
| Control | BI-0153 |
| Recommended cellular usage concentration | 30 – 500 nM |
| In vivo use | Yes |
| Donated by | Boehringer Ingelheim |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | ALOX5AP binding potency: IC50 1.7 nM |
| Selectivity within target family: > 30-fold | Not applicable as no closely related mammalian protein known |
| Selectivity outside target family | Extensive external screens: Invitrogen panel: 546 kinases < 30% inhibition @ 3µM; Panlabs External screen covering 68 targets: @ 10 µM; Cerep External screen covering 137 targets: @ 20 µMClosest off-target in the PDSP scan is SLC6A3 (60.66 % inhibition). |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | ALOX5AP functional inhibition in human whole blood: IC50 45 nM; ALOX5AP functional inhibition in mouse whole blood: IC50 4800 nM |
| Control compound (100 times less potent than the probe) | ALOX5AP: IC50 = 670 nM; PDSP scan: off-target activity for SLC6A3 (Ki = 855.0 nM) |