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Assay Detail

CHEMBL5361626

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

Binding
Antagonist activity at human P2X7 receptor expressed in 1321N1 cells by FLIPR assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321N1
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 8 8.13 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5407113 1 8.62
CHEMBL5440534 1 8.52
CHEMBL5416813 1 8.40
CHEMBL5399698 1 8.24
CHEMBL5411789 1 8.01
CHEMBL5425082 1 7.00
CHEMBL5419802 1 -
CHEMBL5425149 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5407113 IC50 = 2.4 nM 8.62
CHEMBL5440534 IC50 = 3.0 nM 8.52
CHEMBL5416813 IC50 = 4.0 nM 8.40
CHEMBL5399698 IC50 = 5.7 nM 8.24
CHEMBL5411789 IC50 = 9.7 nM 8.01
CHEMBL5425082 IC50 = 100.0 nM 7.00
CHEMBL5419802 IC50 < 10.0 nM -
CHEMBL5425149 IC50 > 100.0 nM -