Compound name
CRTH2
Protein family
GPCR
Target name
PTGDR2
Affinity biochemical (nM)
2.5
Affinity on-target cellular (nM)
3
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000297b
SMILES
CN([C@@H]1CCc2c(CC(=O)O)c3ccccc3n2C1)S(=O)(=O)c1ccc(F)cc1
InChIKey
JTCAGRAKUAAYDY-OAHLLOKOSA-N
NCBI gene ID
11251
UniProt ID
Q9Y5Y4
Synonyms
CRTH2, CD294, DP2
Mode of action
Antagonist
Negative control
CRTH2 negative control
Affinity biochemical definition
Ki
Affinity biochemical assay type
Prostanoid receptor binding assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.bmcl.2010.11.015
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/CRTH%3Csub%3E2%3C/sub%3E%20antagonist
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
cAMP functional assay in HEK-hCRTH2 cells
Affinity on-target cellular relation
=
Selectivity platform
GPCR screen (PDSP)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, closest targets: Ki(SLC6A3) = 283 nM, Ki(GABA/PBR) = 1115 nM, Ki(DRD2) = 3746 nM; Prostanoid receptor binding assay: Ki(TBXA2R)= 3804 nM, >100-fold selective against related receptors; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contrl.: ROCK1 (34%), DYRK1B (44%)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/CRTH%3Csub%3E2%3C/sub%3E%20antagonist
Selectivity Number of Off-targets
0