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Assay Detail

CHEMBL5361616

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

Binding
Inhibition of human P2X7 receptor in HEK cells by fluorescence based calcium influx assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

From lead to clinic: A review of the structural design of P2X7R antagonists.
Zhang R, Li N, Zhao M, Tang M, Jiang X, Cai X, Ye N, Su K, Peng J, Zhang X, Wu W, Ye H.
Eur J Med Chem (2023) 251 : 115234 -115234
PubMed 36893624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.74 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419822 1 8.00
CHEMBL5425828 1 7.77
CHEMBL5221347 1 7.61
CHEMBL340983 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419822 IC50 = 10.0 nM 8.00
CHEMBL5425828 IC50 = 17.0 nM 7.77
CHEMBL5221347 IC50 = 24.5 nM 7.61
CHEMBL340983 IC50 = 25.7 nM 7.59