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Assay Detail

CHEMBL5106947

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

Binding
Antagonist activity at P2X4R (unknown origin) expressed in 1321N1 cells
2
Total Activities
2
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 4 (CHEMBL2104)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2<i>H</i>-naphtho[1,2-<i>b</i>][1,4]diazepine-2,4(3<i>H</i>)-diones as P2X4 Receptor Antagonists.
Toti KS, Verma R, McGonnigle MJ, Gamiotea Turro D, Wen Z, Lewicki SA, Liang BT, Jacobson KA.
J Med Chem (2022) 65 : 13967 -13987
PubMed 36150180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.50 5.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1532400 1 5.71
CHEMBL2180179 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1532400 IC50 = 1950.0 nM 5.71
CHEMBL2180179 IC50 = 5200.0 nM 5.28