TP-051
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Human FFAR1: Ki = 16 nM (FFAR1 Binding Assay) |
| Selectivity within target family: > 30-fold | Closest off targets in the PDSP scan (44 targets) at 10 µM are DDR3 (Ki = 924.7 nM), DDR4 (Ki = 1225.46 nM) and ADRA1D (Ki = 7519.69 nM) |
| Selectivity outside target family | Eurofins Panlabs panel at 10 µM (118 targets): 113 targets > 10 µM; closest off-targets [% inh.]: ALOX5 (85), TBXAS1 (64), EGFR (61), MAPK14 (60), TBXA2R (60) |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: h-FLIPR: EC50 = 25 nM (Functional assay: Ca influx activity of CHO cells) In vitro glucose stimulated insulin secretion assay in INS-1 cells: Maximum effect at 1 µM TP-051 |
| Control compound (100 times less potent than the probe) | TP-051n: Human FFAR1: Ki > 10 µM, h-FLIPR: EC50 > 10 µMSelectivity: Eurofins Panlabs panel at 10 µM (118 targets): 116 targets > 10 µM; closest off-targets [% inh.]: MAPK14 (66), Protein serine/threonine kinase (PKC, non-selective) (-114) PDSP scan (44 targets) at 10 µM clean except for GABA/PBR (Ki = 2752.33 nM) |