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Assay Detail

CHEMBL3238804

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

Binding
Displacement of [3H]cytisine from alpha4/beta2 nAChR (unknown origin)
2
Total Activities
2
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; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.
Crestey F, Jensen AA, Borch M, Andreasen JT, Andersen J, Balle T, Kristensen JL.
J Med Chem (2013) 56 : 9673 -9682
PubMed 24187998 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.62 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293950 1 7.01
CHEMBL442947 ERYSOTRINE 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293950 Ki = 98.0 nM 7.01
CHEMBL442947 ERYSOTRINE Ki = 600.0 nM 6.22