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Assay Detail

CHEMBL829397

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

Binding
Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4
7
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha2/beta4 (CHEMBL2109230)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
Jensen AA, Frølund B, Liljefors T, Krogsgaard-Larsen P.
J Med Chem (2005) 48 : 4705 -4745
PubMed 16033252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.15 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405936 2 5.64
CHEMBL267936 MECAMYLAMINE 4.0 2 5.51
CHEMBL335712 2 5.29
CHEMBL510275 METHYLLYCACONITINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405936 IC50 = 2300.0 nM 5.64
CHEMBL267936 MECAMYLAMINE IC50 = 3100.0 nM 5.51
CHEMBL405936 IC50 = 4000.0 nM 5.40
CHEMBL335712 IC50 = 5100.0 nM 5.29
CHEMBL267936 MECAMYLAMINE IC50 = 16000.0 nM 4.80
CHEMBL335712 IC50 = 57000.0 nM 4.24
CHEMBL510275 METHYLLYCACONITINE IC50 > 1000.0 nM -