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Assay Detail

CHEMBL2344147

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

Binding
Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced Ca2+ flux after 30 mins by FLIPR assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Letavic MA, Lord B, Bischoff F, Hawryluk NA, Pieters S, Rech JC, Sales Z, Velter AI, Ao H, Bonaventure P, Contreras V, Jiang X, Morton KL, Scott B, Wang Q, Wickenden AD, Carruthers NI, Bhattacharya A.
ACS Med Chem Lett (2013) 4 : 419 -422
PubMed 24900687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.00 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2338352 1 8.30
CHEMBL2338351 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2338352 IC50 = 5.012 nM 8.30
CHEMBL2338351 IC50 = 19.95 nM 7.70