T-10430
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: IC50 = 31 nM (Tag-lite assay) |
| Selectivity within target family: > 30-fold | LTB4R , AGTR1: Both show no effect in IP-One assay at up to 50 µM |
| Selectivity outside target family | No activity except for LTB4R2 in GPCR screen (314 receptors, Ca2+ Aequorin assay) at 1 µM |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion:IP-One assay: EC50 = 19.4 nM, cAMP assay: EC50 = 0.51 nM |
| Control compound (100 times less potent than the probe) | T-10404: no effect in IP-One assay at up to 100 µM for LTB4R2 and LTB4R; cAMP assay: EC50 = 560 nM (> 1000 fold) |