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Assay Detail

CHEMBL2184466

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

Functional
Antagonist activity at human P2X3 receptor by cell-based calcium influx assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 3 (CHEMBL2998)
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
IC50 8 5.69 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180149 1 6.37
CHEMBL2180137 1 5.00
CHEMBL2180138 1 -
CHEMBL2180136 1 -
CHEMBL2180174 1 -
CHEMBL2180171 1 -
CHEMBL2180160 1 -
CHEMBL1163419 TNP-ATP 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180149 IC50 = 429.0 nM 6.37
CHEMBL2180137 IC50 = 10000.0 nM 5.00
CHEMBL2180138 IC50 > 10000.0 nM -
CHEMBL2180136 IC50 > 10000.0 nM -
CHEMBL2180174 IC50 >= 10000.0 nM -
CHEMBL2180171 IC50 > 10000.0 nM -
CHEMBL2180160 IC50 > 10000.0 nM -
CHEMBL1163419 TNP-ATP IC50 - -