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Assay Detail

CHEMBL1943867

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

Binding
Displacement of [3H]cytisine from human nAChR alpha2beta4 receptor expressed in human K177 cells
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K177
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent α4β2 nicotinic acetylcholine receptor ligands.
Scanio MJ, Shi L, Bunnelle WH, Anderson DJ, Helfrich RJ, Malysz J, Thorin-Hagene KK, Van Handel CE, Marsh KC, Lee CH, Gopalakrishnan M.
J Med Chem (2011) 54 : 7678 -7692
PubMed 21962147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.80 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127071 POZANICLINE 2.0 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127071 POZANICLINE Ki = 16.0 nM 7.80