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Assay Detail

CHEMBL5134948

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

Binding
Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as reduction in ethidium bromide dye uptake preincubated for 15 mins followed by BzATP addition and measured after 30 mins by Ethidium bromide dye based fluorescence plate reader analysis
3
Total Activities
3
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 7 (CHEMBL4805)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.
Mahmood A, Ali Shah SJ, Iqbal J.
Eur J Med Chem (2022) 231 : 114162 -114162
PubMed 35123298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.27 6.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188202 1 6.81
CHEMBL5184546 1 6.10
CHEMBL5184167 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188202 IC50 = 155.0 nM 6.81
CHEMBL5184546 IC50 = 796.0 nM 6.10
CHEMBL5184167 IC50 = 1259.0 nM 5.90