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Assay Detail

CHEMBL2184475

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Binding
Competitive antagonist activity at human P2X4 receptor expressed in 1321N1 cell membrane assessed as inhibition of [35S]ATPgammaS binding by scintillation counting
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.
Hernandez-Olmos V, Abdelrahman A, El-Tayeb A, Freudendahl D, Weinhausen S, Müller CE.
J Med Chem (2012) 55 : 9576 -9588
PubMed 23075067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.31 7.31
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163419 TNP-ATP 2 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163419 TNP-ATP Ki = 48.9 nM 7.31
CHEMBL1163419 TNP-ATP Inhibition - % -