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Assay Detail

CHEMBL2383618

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

Binding
Displacement of [125I]alpha-bungarotoxin from human alpha7 nAChR overexpressed in human SH-SY5Y cells after 120 mins by liquid scintillation spectrometric analysis
25
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SH-SY5Y
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
Faundez-Parraguez M, Farias-Rabelo N, Gonzalez-Gutierrez JP, Etcheverry-Berrios A, Alzate-Morales J, Adasme-Carreño F, Varas R, Bermudez I, Iturriaga-Vasquez P.
Bioorg Med Chem (2013) 21 : 2687 -2694
PubMed 23561269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.03 5.96
IC50 9 4.73 5.64
Inhibition 7 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381566 3 5.96
CHEMBL3 NICOTINE 4.0 2 5.42
CHEMBL2381563 3 5.35
CHEMBL2381568 3 5.17
CHEMBL2381571 3 4.98
CHEMBL2381564 3 4.53
CHEMBL2381567 2 4.53
CHEMBL2381565 3 4.31
CHEMBL2381570 1 -
CHEMBL2381569 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381566 Ki = 1100.0 nM 5.96
CHEMBL2381566 IC50 = 2300.0 nM 5.64
CHEMBL3 NICOTINE Ki = 3800.0 nM 5.42
CHEMBL2381563 Ki = 4500.0 nM 5.35
CHEMBL2381568 Ki = 6700.0 nM 5.17
CHEMBL3 NICOTINE IC50 = 7600.0 nM 5.12
CHEMBL2381563 IC50 = 8900.0 nM 5.05
CHEMBL2381571 Ki = 10500.0 nM 4.98
CHEMBL2381568 IC50 = 13400.0 nM 4.87
CHEMBL2381571 IC50 = 21100.0 nM 4.68
CHEMBL2381564 Ki = 29300.0 nM 4.53
CHEMBL2381567 Ki = 29500.0 nM 4.53
CHEMBL2381565 Ki = 48700.0 nM 4.31
CHEMBL2381567 IC50 = 59100.0 nM 4.23
CHEMBL2381564 IC50 = 58500.0 nM 4.23
CHEMBL2381565 IC50 = 97300.0 nM 4.01
CHEMBL2381571 Inhibition - % -
CHEMBL2381570 Inhibition - % -
CHEMBL2381563 Inhibition - % -
CHEMBL2381569 Ki = 232000.0 nM -
CHEMBL2381564 Inhibition - % -
CHEMBL2381566 Inhibition - % -
CHEMBL2381569 IC50 = 464000.0 nM -
CHEMBL2381568 Inhibition - % -
CHEMBL2381565 Inhibition - % -