Compound name
BAY-6672
Protein family
GPCR
Target name
PTGFR
Affinity biochemical (nM)
22
Affinity on-target cellular (nM)
11
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001111a
SMILES
Cc1c(N2CCCC2)nc2ccc(Br)cc2c1C(=O)NC[C@H](CCC(=O)O)c1ccccc1Cl.Cl.O
InChIKey
YQOLEILXOBUDMU-KRWDZBQOSA-N
NCBI gene ID
5737
UniProt ID
P43088
Synonyms
FP
Mode of action
Antagonist
Negative control
BAY-403
Affinity biochemical definition
IC50
Affinity biochemical assay type
Panlabs hFP-R binding assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/chemProbes#!specificprobeoverview/BAY-6672
Affinity biochemical relation
0
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Human FP-R assay (Chem-1 cells expressing human FP receptor, Eurofins)
Affinity on-target cellular source knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00834
Affinity on-target cellular relation
0
Selectivity platform
GPCR panel (PDSP screen)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, closest target as % of inhibition: HTR3A (38%); Screened against other human prostanoid receptor (binding assay, Eurofins/Panlabs): IC50(PTGFR) = 22 nM, IC50(EP1) >10 µM, IC50(EP2) >10 µM, IC50(EP3) >10 µM, IC50(EP4) >10 µM, IC50(IP) >10 µM, IC50(DP) >10 µM, IC50(CRTH2) >10 µM, >420-fold selective; Screened in cell-based assay (Eurofins/Panlabs): IC50(TBXA2R) = 2.2 µM, 200-fold selective; Screened at 10 µM against 77 other targets (Leadprofiling Screen, Panlabs), closest target as % of inhibition: TBXAS1 (33%); Screened at 10 µM against 8 ion channels (Ion channel profiler, Eurofins): IC20(Nav1.5) >10 μM, IC20(Kv4.3/KChIP2) >10 μM, IC20(Cav1.2) >10 μM, IC20(Kv1.5) >10 μM, IC20(KCNQ/minK) >10 μM, IC20(herG) >10 μM, IC20(HCN4) >10 μM, IC20(Kir2.1) >10 μM
Selectivity Source Knowledge
https://pubs.acs.org/doi/10.1021/acs.jmedchem.0c00834
Selectivity Number of Off-targets
0