Compound name
TP-051
Protein family
GPCR
Target name
FFAR1
Affinity biochemical (nM)
16
Affinity on-target cellular (nM)
25
CG-Set
GPCR set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001554a
SMILES
Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1
InChIKey
RPAHCZZXEGWBDL-UHFFFAOYSA-N
NCBI gene ID
2864
UniProt ID
O14842
Synonyms
FFA1R
Mode of action
agonist
Negative control
TP-051n
Affinity biochemical definition
Ki
Affinity biochemical assay type
Radiometric GPR40 receptor binding assay
Affinity Biochemical Source Knowledge
https://pubs.acs.org/doi/10.1021/jm2016123
Affinity biochemical relation
0
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
FLIPR assay (Ca influx activity of CHO cells expressing human GPR40)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/10.1021/jm2016123
Affinity on-target cellular relation
0
Selectivity platform
Eurofins Panlabs panel
Selectivity platform number of targets
118
Selectivity remarks
Screened at 10 µM, closest targets as % of inhibition: ALOX5 (85%), TBXAS1 (64%), EGFR (61%), MAPK14 (60%), TBXA2R (60%), others >10 µM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/TP-051
Selectivity Number of Off-targets
0