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TP-051

2D structure
Target FFAR1 
Targeted domain Pocket between TM1 and TM3
Mode of action Agonist
Control TP-051n
Orthogonal probe BI-2081 
Recommended cellular usage concentration ≤ 1 µM
In vivo use Yes
Synonyms Compound 31
Donated by Takeda


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 µM
Selectivity: 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)