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

CHEMBL755477

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

Binding
In vitro binding affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membrane using [3H]cytisine as radioligand
25
Total Activities
25
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; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.
Nielsen SF, Nielsen EO, Olsen GM, Liljefors T, Peters D.
J Med Chem (2000) 43 : 2217 -2226
PubMed 10841800 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.89 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59986 1 8.82
CHEMBL72789 1 8.74
CHEMBL71085 1 8.72
CHEMBL71666 1 8.72
CHEMBL74068 1 8.66
CHEMBL72320 1 8.62
CHEMBL72262 1 8.62
CHEMBL70335 1 8.55
CHEMBL303889 1 8.52
CHEMBL72605 1 8.52
CHEMBL304604 1 8.40
CHEMBL71255 1 8.40
CHEMBL72284 1 8.35
CHEMBL69725 1 8.18
CHEMBL62765 1 8.17
CHEMBL72523 1 8.10
CHEMBL70737 1 7.70
CHEMBL273218 1 7.00
CHEMBL70717 1 6.77
CHEMBL71068 1 6.77
CHEMBL71067 1 6.77
CHEMBL9965 1 6.72
CHEMBL74466 1 6.66
CHEMBL68563 1 6.51
CHEMBL305073 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59986 IC50 = 1.5 nM 8.82
CHEMBL72789 IC50 = 1.8 nM 8.74
CHEMBL71085 IC50 = 1.9 nM 8.72
CHEMBL71666 IC50 = 1.9 nM 8.72
CHEMBL74068 IC50 = 2.2 nM 8.66
CHEMBL72320 IC50 = 2.4 nM 8.62
CHEMBL72262 IC50 = 2.4 nM 8.62
CHEMBL70335 IC50 = 2.8 nM 8.55
CHEMBL303889 IC50 = 3.0 nM 8.52
CHEMBL72605 IC50 = 3.0 nM 8.52
CHEMBL304604 IC50 = 4.0 nM 8.40
CHEMBL71255 IC50 = 4.0 nM 8.40
CHEMBL72284 IC50 = 4.5 nM 8.35
CHEMBL69725 IC50 = 6.6 nM 8.18
CHEMBL62765 IC50 = 6.7 nM 8.17
CHEMBL72523 IC50 = 8.0 nM 8.10
CHEMBL70737 IC50 = 20.0 nM 7.70
CHEMBL273218 IC50 = 100.0 nM 7.00
CHEMBL70717 IC50 = 170.0 nM 6.77
CHEMBL71068 IC50 = 170.0 nM 6.77
CHEMBL71067 IC50 = 170.0 nM 6.77
CHEMBL9965 IC50 = 190.0 nM 6.72
CHEMBL74466 IC50 = 220.0 nM 6.66
CHEMBL68563 IC50 = 310.0 nM 6.51
CHEMBL305073 IC50 = 500.0 nM 6.30