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Assay Detail

CHEMBL5365098

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Binding
Antagonist activity at human P2X7 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, Synthesis, and Biological Evaluation of Novel P2X7 Receptor Antagonists for the Treatment of Septic Acute Kidney Injury.
Zhang R, Su K, Yang L, Tang M, Zhao M, Ye N, Cai X, Jiang X, Li N, Peng J, Zhang X, Wang B, Wu W, Ma L, Ye H.
J Med Chem (2023) 66 : 11365 -11389
PubMed 37582195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.47 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4159914 1 8.52
CHEMBL4162056 1 8.28
CHEMBL5394275 1 7.96
CHEMBL3697519 1 7.88
CHEMBL271462 1 7.80
CHEMBL5221347 1 7.61
CHEMBL5205239 1 7.47
CHEMBL5425082 1 7.00
CHEMBL5400871 1 6.99
CHEMBL5440566 1 6.70
CHEMBL5440646 1 5.96
CHEMBL5411194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4159914 IC50 = 3.0 nM 8.52
CHEMBL4162056 IC50 = 5.3 nM 8.28
CHEMBL5394275 IC50 = 11.1 nM 7.96
CHEMBL3697519 IC50 = 13.3 nM 7.88
CHEMBL271462 IC50 = 15.85 nM 7.80
CHEMBL5221347 IC50 = 24.5 nM 7.61
CHEMBL5205239 IC50 = 34.0 nM 7.47
CHEMBL5425082 IC50 = 100.0 nM 7.00
CHEMBL5400871 IC50 = 103.0 nM 6.99
CHEMBL5440566 IC50 = 199.5 nM 6.70
CHEMBL5440646 IC50 = 1100.0 nM 5.96
CHEMBL5411194 IC50 < 50.0 nM -