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Assay Detail

CHEMBL3057497

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

Binding
Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin)
5
Total Activities
5
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

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 5 8.81 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59986 1 10.40
CHEMBL6623 EPIBATIDINE 1 10.15
CHEMBL3 NICOTINE 4.0 1 8.98
CHEMBL2261113 1 8.40
CHEMBL2261114 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59986 Ki = 0.04 nM 10.40
CHEMBL6623 EPIBATIDINE Ki = 0.07 nM 10.15
CHEMBL3 NICOTINE Ki = 1.05 nM 8.98
CHEMBL2261113 Ki = 4.0 nM 8.40
CHEMBL2261114 Ki = 734.0 nM 6.13