Compound name
BI-2081
Protein family
GPCR
Target name
FFAR1
Affinity biochemical (nM)
23
Affinity on-target cellular (nM)
3
CG-Set
GPCR set
Recommended Concentration
200 nM
Compound EUbOPEN ID
EUB0001718a
SMILES
Cc1cc(OCCC(C)(C)O)cc(C)c1-c1ccc(F)c2c1CC[C@H]2Oc1ccc2c(c1)OC[C@H]2CC(=O)O
InChIKey
VXNAMCLMCBLNOL-NFQMXDRXSA-N
NCBI gene ID
2864
UniProt ID
O14842
Synonyms
FFA1R
Mode of action
Agonist
Negative control
BI-0340
Affinity biochemical definition
Ki
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/BI-2081
Affinity biochemical relation
=
Affinity on-target cellular definition
EC50
Affinity on-target cellular assay type
Human IPOne assay (Stimulation of 1321N1 cells, which express the GPR40 receptor, followed by measurement of the IP1 accumulation by fluorescence)
Affinity on-target cellular source knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!detailedpotencydataview/BI-2081
Affinity on-target cellular relation
=
Selectivity platform
SafetyScreen44™ (Eurofins)
Selectivity platform number of targets
44
Selectivity remarks
Screened at 10 µM against a panel of GPCRs, ion channels, and other enzymes, closest targets as % of control: ALPHA2 (5.5%), PPARG (8%), ALPHA2C (23%), full screening data available on Open Me website, https://www.opnme.com/molecules/gpr40-agonist-bi-2081;
Selectivity Source Knowledge
https://www.opnme.com/molecules/gpr40-agonist-bi-2081
Selectivity Number of Off-targets
2