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Assay Detail

CHEMBL3766467

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

Binding
Agonist activity at human alpha7 receptor expressed in mouse Neuro2a cells assessed as induction of intracellular calcium level preincubated with PNU-120596 for 20 mins followed by compound addition measured every 2 sec for 3 mins by fluorescence microplate reader analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Neuro2a
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New quinoline derivatives as nicotinic receptor modulators.
Manetti D, Bellucci C, Dei S, Teodori E, Varani K, Spirova E, Kudryavtsev D, Shelukhina I, Tsetlin V, Romanelli MN.
Eur J Med Chem (2016) 110 : 246 -258
PubMed 26840365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.87 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764496 1 5.96
CHEMBL3763220 1 5.85
CHEMBL3765305 1 5.80
CHEMBL3764445 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764496 EC50 = 1090.0 nM 5.96
CHEMBL3763220 EC50 = 1410.0 nM 5.85
CHEMBL3765305 EC50 = 1570.0 nM 5.80
CHEMBL3764445 EC50 - -