EUB0000274bCl_P2RY14

Chemical structure of compound EUB0000274bCl
Compound name
PPTN
Protein family
GPCR
Target name
P2RY14
Affinity biochemical (nM)
0.5
Affinity on-target cellular (nM)
7.96
CG-Set
GPCR set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000274bCl
SMILES
Cl.O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1
InChIKey
FKMVYPCBLWYNAV-UHFFFAOYSA-N
NCBI gene ID
9934
UniProt ID
Q15391
Synonyms
KIAA0001
Mode of action
Antagonist
Negative control
PPTN-NC
Affinity biochemical definition
IC50
Affinity biochemical assay type
FLIPR assay
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PPTN
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Fluorescence binding assay (using flow cytometry in hP2Y14R-expressing CHO cells)
Affinity on-target cellular relation
=
Selectivity platform
GPCR screen (PDSP)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, >10,000-fold selectivity over other P2RY* receptors, closest targets: Ki(DRD3) = 884.3 nM, Ki(TMEM97) = 1120.99 nM, Ki(SIGMAR1) = 1180.59 nM, Ki(ADRA2B) = 2561.53 nM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest target: MAPKAPK2 (51% of contr.); Screened in Eurofins-Panlabs enzyme assay against 40 targets at 10 µM, closest targets: IC50(INSR) = 4.31 µM, IC50(EGFR) = 4.59 µM; Screened in Eurofins-Panlabs radioligand binding assay against 125 targets at 1 µM and 10 µM, closest targets: IC50(CYSLTR1) = 560 nM, IC50(HRH2) = 1390 nM, IC50(SLC6A3) = 2310 nM; Screened in PDSP screen against 45 receptors, ion channels and transporters at 10 µM, closest targets: Ki(D3 dopamine receptor) = 6.79 µM, Ki(d-opioid receptor) = 2.75 µM
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.8b00168
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PPTN
Selectivity Number of Off-targets
0