Compound name
BAY-1797
Protein family
P2X receptors
Target name
P2RX4
Affinity on-target cellular (nM)
211
CG-Set
Ion Channel
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000309b
SMILES
NS(=O)(=O)c1cc(NC(=O)Cc2ccccc2)ccc1Oc1cccc(Cl)c1
InChIKey
CSJYMAFXYMYNCK-UHFFFAOYSA-N
NCBI gene ID
5025
UniProt ID
Q99571
Synonyms
P2RX4
Mode of action
Inhibitor
Negative control
BAY-207
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
FLIPR assay (inhibition of ATP-induced calcium influx in HEK cells, stably transfected with human P2X4 receptor)
Affinity on-target cellular relation
=
Selectivity platform
Lead profiling screen (Eurofins)
Selectivity platform number of targets
67
Selectivity remarks
Screened against 67 GPCRs, ion channels, kinases and transporters at 10 µM, closest targets: IC50(SLC6A3) = 2.17 µM, IC50(P2RX1) >50 µM, IC50(P2RX2) >30 µM, IC50(P2RX3) = 8.3 µM, IC50(P2RX7) = 10.6 µM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: WNK2 (0%), WNK4 (0%), BUB1 (1.6%), EGFR(L747-T751del,Sins) (47%); Screened against 45 GPCR targets at 10 µM (PDPS screen), closest targets: Ki(TMEM97) = 4.34 µM, Ki(ADRA2B) = 4.58 µM, Ki(HTR2C) = 6.52 µM;
Selectivity Source Knowledge
https://doi.org/10.1021/acs.jmedchem.9b01304
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BAY-1797
Selectivity Number of Off-targets
0