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Assay Detail

CHEMBL754454

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

Functional
Antagonist activity against recombinant human P2X purinoceptor 7 (P2X7)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

P2X purinoceptor 7 (CHEMBL4805)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Purine and pyrimidine (P2) receptors as drug targets.
Jacobson KA, Jarvis MF, Williams M.
J Med Chem (2002) 45 : 4057 -4093
PubMed 12213051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 5.26 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28324 1 7.47
CHEMBL339386 1 4.28
CHEMBL265502 SURAMIN 3.0 1 4.04
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER 1 -
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28324 EC50 = 34.0 nM 7.47
CHEMBL339386 EC50 = 52000.0 nM 4.28
CHEMBL265502 SURAMIN EC50 = 92000.0 nM 4.04
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER EC50 > 100000.0 nM -
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 780000.0 nM -