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Assay Detail

CHEMBL4054683

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

Binding
Antagonist activity at P2X7 in human whole blood assessed as inhibition of BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP addition measured after 1.5 hrs by ELISA
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

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.
J Med Chem (2017) 60 : 4559 -4572
PubMed 28493698 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4079239 JNJ-54175446 2.0 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4079239 JNJ-54175446 IC50 = 7.943 nM 8.10