BI 99179
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, KD) | Inhibition of FASN: IC50 = 0.079 µM |
| Selectivity within target family: > 30-fold | No closely related mammalian proteins as potential off-targets |
| Selectivity outside target family | External screen covering 30 non-related targets: <20% inhibition @ 10 µM for all targetsThe only hit in the PDSP scan is SLC6A3 (77.27 % inhibition). |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | 1. Inhibition of [14C]acetate incorporation into mouse N-42 cells: IC50 = 0.57 µM 2. Inhibition of [14C]acetate incorporation into human H1975 cells: IC50 = 0.18 µM |
| Control compound (100 times less potent than the probe) | Inhibition of FASN: >3 µM for inactive analog BI 99990; Shows weak off-target activity in the PDSP scan for TMEM97 (Sigma2) (Ki = 396.0 nM) and HRH4 (Ki = 1635.0 nM). |