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Assay Detail

CHEMBL3606542

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

Binding
Antagonist activity against human P2X7 receptor assessed as inhibition of IL-1beta production by cell based assay
1
Total Activities
1
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

Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.
Rudolph DA, Alcazar J, Ameriks MK, Anton AB, Ao H, Bonaventure P, Carruthers NI, Chrovian CC, De Angelis M, Lord B, Rech JC, Wang Q, Bhattacharya A, Andres JI, Letavic MA.
Bioorg Med Chem Lett (2015) 25 : 3157 -3163
PubMed 26099534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.85 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823817 CE-224535 2.0 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823817 CE-224535 IC50 = 1.4 nM 8.85