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Assay Detail

CHEMBL2184469

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Functional
Antagonist activity at mouse P2X4 receptor by cell-based calcium influx assay
10
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 4 (CHEMBL2176849)
Type SINGLE PROTEIN
Organism Mus musculus

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 5.68 5.89
EC50 2 5.50 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 6.00
CHEMBL1163419 TNP-ATP 1 5.89
CHEMBL2180137 1 5.75
CHEMBL2180160 1 5.75
CHEMBL2180149 1 5.58
CHEMBL2180174 1 5.57
CHEMBL2180138 1 5.55
CHEMBL336208 1 5.00
CHEMBL2180136 1 -
CHEMBL2180171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 1000.0 nM 6.00
CHEMBL1163419 TNP-ATP IC50 = 1280.0 nM 5.89
CHEMBL2180137 IC50 = 1770.0 nM 5.75
CHEMBL2180160 IC50 = 1760.0 nM 5.75
CHEMBL2180149 IC50 = 2660.0 nM 5.58
CHEMBL2180174 IC50 = 2710.0 nM 5.57
CHEMBL2180138 IC50 = 2810.0 nM 5.55
CHEMBL336208 EC50 = 10000.0 nM 5.00
CHEMBL2180136 IC50 > 10000.0 nM -
CHEMBL2180171 IC50 > 10000.0 nM -