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Assay Detail

CHEMBL3057495

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

Binding
Displacement of [3H]nicotine from Homo sapiens (human) alpha4beta2 nicotinic acetylcholine receptor expressed in Homo sapiens (human) SH-EP1 cells after 2.5 min by scintillation counting
7
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-EP1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Biososteric Replacement in the Design and Synthesis of Ligands for Nicotinic Acetylcholine Receptors
Sun W, Blanton MP, Gabriel JL, Canney DJ
Med Chem Res (2005) 14 : 241 -259
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.95 6.52
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61616 1 6.52
CHEMBL2261108 1 6.44
CHEMBL113076 1 6.35
CHEMBL2261107 1 5.47
CHEMBL2261111 2 4.95
CHEMBL2261112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61616 Ki = 300.0 nM 6.52
CHEMBL2261108 Ki = 360.0 nM 6.44
CHEMBL113076 Ki = 450.0 nM 6.35
CHEMBL2261107 Ki = 3390.0 nM 5.47
CHEMBL2261111 Ki = 11200.0 nM 4.95
CHEMBL2261111 Inhibition - % -
CHEMBL2261112 Ki - -