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Assay Detail

CHEMBL990849

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

Binding
Displacement of [3H]epibatidine from rat alpha6beta2 nAChR expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-6 (CHEMBL4747)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.
Gao Y, Kuwabara H, Spivak CE, Xiao Y, Kellar K, Ravert HT, Kumar A, Alexander M, Hilton J, Wong DF, Dannals RF, Horti AG.
J Med Chem (2008) 51 : 4751 -4764
PubMed 18605717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 10.14 10.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL476140 1 10.68
CHEMBL514372 1 10.51
CHEMBL478029 1 10.33
CHEMBL478447 1 9.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL476140 Ki = 0.021 nM 10.68
CHEMBL514372 Ki = 0.031 nM 10.51
CHEMBL478029 Ki = 0.047 nM 10.33
CHEMBL478447 Ki = 0.95 nM 9.02