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Assay Detail

CHEMBL5554641

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

Binding
Antagonist activity at human P2X3 receptor expressed in HEK293 cells preincubated for 30 mins followed by alpha, beta me-ATP addition and measured for 10 mins by Fluo-8 dye based FLIPR assay
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 3 (CHEMBL2998)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Triazolopyrimidine Derivatives as Selective P2X3 Receptor Antagonists Binding to an Unprecedented Allosteric Site as Evidenced by Cryo-Electron Microscopy.
Kim GR, Kim S, Kim YO, Han X, Nagel J, Kim J, Song DI, Müller CE, Yoon MH, Jin MS, Kim YC.
J Med Chem (2024) 67 : 14443 -14465
PubMed 39102524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.60 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5207245 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5207245 IC50 = 25.0 nM 7.60