IPP/CNRS-A017
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd>/sub>) | Surpasses criterion: IC50= 25 nM (activity assay) |
| Selectivity within target family: > 30-fold | Surpasses criterion: No related human family members. |
| Selectivity outside target family | PDSP screen (44 targets): Closest off-targets at 10 µM are GABA/ PBR (KD =2.1 µM), ADRA1D (KD = 4.1 µM) and TMEM97 (KD = 583 nM)PDSP GPCR screen: Closest off-targets are TMEM97 (83.71 % inhibition), ADRA2A (77.67 % inhibition), GABA/PBR (62.49 % inhibition) and ADRB3 (Ki = 5327.21 nM).Clean KINOMEscan. |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: IC50 = 2.5 nM (HEK293 measle assay) |
| Control compound (100 times less potent than the probe) | Surpasses criterion: IC50 = 1.2 µM (measles assay) (480 fold); Clean PDSP scan except for one hit: TMEM97 (Ki = 5252.78 nM) |