Compound name
TP-051n
Protein family
GPCR
Target name
FFAR1
Affinity biochemical (nM)
10000
Affinity on-target cellular (nM)
10000
CG-Set
GPCR set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001555
SMILES
Cc1cc(OC2CCS(=O)(=O)CC2)cc(C)c1-c1cccc(COc2ccc(C(=O)O)c(F)c2)c1
InChIKey
OLFCZVVFPNDHIW-UHFFFAOYSA-N
NCBI gene ID
2864
UniProt ID
O14842
Synonyms
FFA1R
Mode of action
Negative control for TP-051
Affinity biochemical definition
Ki
Affinity biochemical assay type
Radiometric GPR40 receptor binding assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/TP-051
Affinity biochemical relation
>
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://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/TP-051
Affinity on-target cellular relation
>
Selectivity platform
Eurofins Panlabs panel
Selectivity platform number of targets
118
Selectivity remarks
Screened at 10 µM, closest targets as % of inhibition: LYN (70%), MAPK14 (66%), PKC non-selective (-114%), others >10 µM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/TP-051
Selectivity Number of Off-targets
0