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Assay Detail

CHEMBL1826114

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

Binding
Displacement of [3H]-epibatidine from alpha3beta4 nAChR expressed in human IMR32 cells after 2 hrs by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type IMR-32
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and biological activity of a novel class nicotinic acetylcholine receptors (nAChRs) ligands structurally related to anatoxin-a.
Simoni D, Rondanin R, Marchetti P, Rullo C, Baruchello R, Grisolia G, Barbato G, Giovannini R, Marchioro C, Capelli AM, Virginio C, Bozzoli A, Borea PA, Merighi S, Donati D.
Bioorg Med Chem Lett (2011) 21 : 5423 -5427
PubMed 21824774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.76 5.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823382 1 5.98
CHEMBL1823380 1 5.75
CHEMBL1823381 1 5.54
CHEMBL1823379 1 -
CHEMBL1823383 1 -
CHEMBL1823384 1 -
CHEMBL1823385 1 -
CHEMBL1823386 1 -
CHEMBL1823387 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823382 IC50 = 1050.0 nM 5.98
CHEMBL1823380 IC50 = 1800.0 nM 5.75
CHEMBL1823381 IC50 = 2900.0 nM 5.54
CHEMBL1823379 IC50 > 10000.0 nM -
CHEMBL1823383 IC50 > 10000.0 nM -
CHEMBL1823384 IC50 > 10000.0 nM -
CHEMBL1823385 IC50 > 10000.0 nM -
CHEMBL1823386 IC50 > 10000.0 nM -
CHEMBL1823387 IC50 > 10000.0 nM -