Compound name
BAY-386
Protein family
GPCR
Target name
F2R
Affinity biochemical (nM)
56
Affinity on-target cellular (nM)
10
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000291b
SMILES
O=C(N1CCS(=O)(=O)CC1)N1C[C@@](S)(c2ccc(OC(F)(F)F)cc2)C[C@@](S)(c2nc(C3CC3)no2)C1
InChIKey
FWONKSVKZWQNPN-RTWAWAEBSA-N
NCBI gene ID
2149
UniProt ID
P25116
Synonyms
TR, CF2R, PAR1, PAR-1
Mode of action
Antagonist
Negative control
BAY-448
Affinity biochemical definition
IC50
Affinity biochemical assay type
Binding assay (platelet membranes)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-386
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Functional cellular assay in HEK cells expressing F2R
Affinity on-target cellular relation
=
Selectivity platform
Eurofins-Panlabs radioligand binding assay
Selectivity platform number of targets
68
Selectivity remarks
Screened at 10 µM, closest target as % of inhibition: CNR1 (88 %); CNR1 functional test (GTPyS binding): IC50 = 10.6 µM; Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki(TMEM97) = 1203.22 nM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: CDK11A (0%), DCLK2(0%), MAP3K12(0%), CDK18(0%), CDK4(18%), TYK2(53%);
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-386
Selectivity Number of Off-targets
0