Compound name
PF-04418948
Protein family
GPCR
Target name
PTGER2
Affinity biochemical (nM)
5
Affinity on-target cellular (nM)
1.8
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000351a
SMILES
COC1=CC2=C(C=C(OCC3(C(O)=O)CN(C(C4=CC=C(F)C=C4)=O)C3)C=C2)C=C1
InChIKey
LWJGMYMNSNVCEM-UHFFFAOYSA-N
NCBI gene ID
5732
UniProt ID
P43116
Synonyms
EP2
Mode of action
Antagonist
Negative control
PF-04475866
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic inhibition assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04418948
Affinity biochemical relation
=
Affinity on-target cellular definition
Kd
Affinity on-target cellular assay type
Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)
Affinity on-target cellular relation
=
Selectivity platform
GPCR screen (PDSP)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, no target >50% of inhibition; F-04418948 displayed >2000-fold functional selectivity for the human EP2 receptor over antagonist activity against the human EP1, EP3, EP4, DP1 and CRTH2 receptors; Selectivity over human IP, FP, TP and LTB4 receptors; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: PRKAA2 (28%), TAOK3 (35%), PIK3CA (42%); Screened in CEREP ligand profiling (at 10 µM, against 125 targets), closest targets: IC50(NQO2) = 0.53 µM, IC50(PDE3) = 3.5 µM, IC50(LTB4R) = 9.7 µM
Selectivity Source Knowledge
https://doi.org/10.1111/j.1476-5381.2011.01495.x
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-04418948
Selectivity Number of Off-targets
0