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Assay Detail

CHEMBL824055

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Binding
binding affinity in rat hippocampi against alpha7 nicotinic receptor
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
Mullen G, Napier J, Balestra M, DeCory T, Hale G, Macor J, Mack R, Loch J, Wu E, Kover A, Verhoest P, Sampognaro A, Phillips E, Zhu Y, Murray R, Griffith R, Blosser J, Gurley D, Machulskis A, Zongrone J, Rosen A, Gordon J.
J Med Chem (2000) 43 : 4045 -4050
PubMed 11063601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.41 7.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293975 2 7.04
CHEMBL193016 1 6.72
CHEMBL129932 3 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293975 Ki = 92.0 nM 7.04
CHEMBL193016 Ki = 190.0 nM 6.72
CHEMBL129932 Ki = 220.0 nM 6.66
CHEMBL129932 Ki = 250.0 nM 6.60
CHEMBL293975 Ki = 9400.0 nM 5.03
CHEMBL129932 Ki > 32000.0 nM -