Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL750053

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

Binding
Inhibitory activity against nicotinic acetylcholine receptor alpha3-beta4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure activity studies of ring E analogues of methyllycaconitine. Part 2: Synthesis of antagonists to the alpha3beta4* nicotinic acetylcholine receptors through modifications to the ester.
Bergmeier SC, Ismail KA, Arason KM, McKay S, Bryant DL, McKay DB.
Bioorg Med Chem Lett (2004) 14 : 3739 -3742
PubMed 15203153 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.35 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267936 MECAMYLAMINE 4.0 1 7.00
CHEMBL1687 1 5.70
CHEMBL121721 HEXAMETHONIUM HYDROXIDE 1 -
CHEMBL1190 DECAMETHONIUM 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267936 MECAMYLAMINE IC50 = 100.0 nM 7.00
CHEMBL1687 IC50 = 2000.0 nM 5.70
CHEMBL121721 HEXAMETHONIUM HYDROXIDE IC50 ~ 1700.0 nM -
CHEMBL1190 DECAMETHONIUM IC50 ~ 1700.0 nM -