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Assay Detail

CHEMBL828851

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

Binding
Inhibition of [3H]cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
6
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Corrigendum to Epibatidine structureactivity relationships
Carroll FI
Bioorg Med Chem Lett (2004) 14 : 5713 -5713
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 9.17 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186302 1 10.52
CHEMBL6623 EPIBATIDINE 2 10.40
CHEMBL361298 1 9.33
CHEMBL185667 1 8.18
CHEMBL363973 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186302 Ki = 0.03 nM 10.52
CHEMBL6623 EPIBATIDINE Ki = 0.04 nM 10.40
CHEMBL361298 Ki = 0.47 nM 9.33
CHEMBL6623 EPIBATIDINE Ki = 0.9 nM 9.05
CHEMBL185667 Ki = 6.6 nM 8.18
CHEMBL363973 Ki = 30.0 nM 7.52