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Assay Detail

CHEMBL5055824

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

Binding
Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced current at -60 mV by whole cell QPatch electrophysiology
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2X purinoceptor 7 (CHEMBL2496)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Hopper AT, Juhl M, Hornberg J, Badolo L, Kilburn JP, Thougaard A, Smagin G, Song D, Calice L, Menon V, Dale E, Zhang H, Cajina M, Nattini ME, Gandhi A, Grenon M, Jones K, Khayrullina T, Chandrasena G, Thomsen C, Zorn SH, Brodbeck R, Poda SB, Staal R, Möller T.
J Med Chem (2021) 64 : 4891 -4902
PubMed 33822617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.18 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5086274 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5086274 IC50 = 66.0 nM 7.18