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Assay Detail

CHEMBL828849

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

Binding
Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
9
Total Activities
6
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 9 9.89 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 2 10.70
CHEMBL186302 1 10.40
CHEMBL186070 1 10.30
CHEMBL426974 3 9.89
CHEMBL185667 1 -
CHEMBL363973 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.02 nM 10.70
CHEMBL186302 Ki = 0.04 nM 10.40
CHEMBL186070 Ki = 0.05 nM 10.30
CHEMBL426974 Ki = 0.13 nM 9.89
CHEMBL6623 EPIBATIDINE Ki = 0.26 nM 9.59
CHEMBL426974 Ki = 0.35 nM 9.46
CHEMBL426974 Ki = 1.25 nM 8.90
CHEMBL185667 Ki > 38.0 nM -
CHEMBL363973 Ki > 38.0 nM -