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Assay Detail

CHEMBL749346

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Binding
Alpha 7 nicotinic acetylcholine receptor binding activity in PC12 cells
15
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type PC-12
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

(+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane as potent agonists for the alpha7 nicotinic acetylcholine receptor.
Tatsumi R, Seio K, Fujio M, Katayama J, Horikawa T, Hashimoto K, Tanaka H.
Bioorg Med Chem Lett (2004) 14 : 3781 -3784
PubMed 15203161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.66 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL330789 3 7.64
CHEMBL125069 1 7.58
CHEMBL339774 1 7.23
CHEMBL122091 1 6.96
CHEMBL420156 3 6.89
CHEMBL124899 1 6.43
CHEMBL121877 1 6.29
CHEMBL331299 1 6.12
CHEMBL122440 1 6.02
CHEMBL125092 1 5.77
CHEMBL121932 BENZOCLIDINE 2.0 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL330789 IC50 = 23.0 nM 7.64
CHEMBL125069 IC50 = 26.0 nM 7.58
CHEMBL339774 IC50 = 59.0 nM 7.23
CHEMBL330789 IC50 = 65.0 nM 7.19
CHEMBL122091 IC50 = 110.0 nM 6.96
CHEMBL420156 IC50 = 130.0 nM 6.89
CHEMBL420156 IC50 = 150.0 nM 6.82
CHEMBL420156 IC50 = 170.0 nM 6.77
CHEMBL330789 IC50 = 220.0 nM 6.66
CHEMBL124899 IC50 = 370.0 nM 6.43
CHEMBL121877 IC50 = 515.0 nM 6.29
CHEMBL331299 IC50 = 760.0 nM 6.12
CHEMBL122440 IC50 = 950.0 nM 6.02
CHEMBL125092 IC50 = 1700.0 nM 5.77
CHEMBL121932 BENZOCLIDINE IC50 = 2600.0 nM 5.58