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Assay Detail

CHEMBL839976

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 in rat cortex
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Coe JW, Vetelino MG, Bashore CG, Wirtz MC, Brooks PR, Arnold EP, Lebel LA, Fox CB, Sands SB, Davis TI, Schulz DW, Rollema H, Tingley FD, O'Neill BT.
Bioorg Med Chem Lett (2005) 15 : 2974 -2979
PubMed 15908213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.02 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 9.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 0.95 nM 9.02