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Assay Detail

CHEMBL4324809

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Antagonist activity at human P2X4 receptor tranfected in human HEK293 cells assessed as inhibition of ATP-induced calcium influx by Fluo2-AM staining based inverted fluorescence microscopic method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 4 (CHEMBL2104)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of the Potent and Selective P2X4 Inhibitor <i>N</i>-[4-(3-Chlorophenoxy)-3-sulfamoylphenyl]-2-phenylacetamide (BAY-1797) and Structure-Guided Amelioration of Its CYP3A4 Induction Profile.
Werner S, Mesch S, Hillig RC, Ter Laak A, Klint J, Neagoe I, Laux-Biehlmann A, Dahllöf H, Bräuer N, Puetter V, Nubbemeyer R, Schulz S, Bairlein M, Zollner TM, Steinmeyer A.
J Med Chem (2019) 62 : 11194 -11217
PubMed 31746599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.11 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1532400 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1532400 IC50 = 780.0 nM 6.11