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Assay Detail

CHEMBL1785674

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

Binding
Displacement of [125I]epibatidine from alpha4beta2* nAChR in C57BL/6J mouse cortical membrane by gamma counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Nicotinic acetylcholine receptor alpha-4/beta-2 (CHEMBL3301382)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Breining SR, Bencherif M, Grady SR, Whiteaker P, Marks MJ, Wageman CR, Lester HA, Yohannes D.
Bioorg Med Chem Lett (2009) 19 : 4359 -4363
PubMed 19560354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.96 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217150 1 9.30
CHEMBL1783888 1 8.92
CHEMBL1783886 1 8.74
CHEMBL3215819 1 8.01
CHEMBL1783883 1 7.96
CHEMBL1783881 1 7.80
CHEMBL1782074 1 7.70
CHEMBL1783884 1 7.62
CHEMBL1783879 1 7.60
CHEMBL1783878 1 7.52
CHEMBL1783882 1 7.23
CHEMBL1783880 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217150 Ki = 0.5 nM 9.30
CHEMBL1783888 Ki = 1.2 nM 8.92
CHEMBL1783886 Ki = 1.8 nM 8.74
CHEMBL3215819 Ki = 9.8 nM 8.01
CHEMBL1783883 Ki = 11.0 nM 7.96
CHEMBL1783881 Ki = 16.0 nM 7.80
CHEMBL1782074 Ki = 20.0 nM 7.70
CHEMBL1783884 Ki = 24.0 nM 7.62
CHEMBL1783879 Ki = 25.0 nM 7.60
CHEMBL1783878 Ki = 30.0 nM 7.52
CHEMBL1783882 Ki = 59.0 nM 7.23
CHEMBL1783880 Ki = 69.0 nM 7.16