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Assay Detail

CHEMBL870896

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

ADMET
Inhibition of CYP2D6
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(R)-3'-(3-methylbenzo[b]thiophen-5-yl)spiro[1-azabicyclo[2,2,2]octane-3,5'-oxazolidin]-2'-one, a novel and potent alpha7 nicotinic acetylcholine receptor partial agonist displays cognitive enhancing properties.
Tatsumi R, Fujio M, Takanashi S, Numata A, Katayama J, Satoh H, Shiigi Y, Maeda J, Kuriyama M, Horikawa T, Murozono T, Hashimoto K, Tanaka H.
J Med Chem (2006) 49 : 4374 -4383
PubMed 16821797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.14 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192704 1 5.70
CHEMBL213024 1 5.05
CHEMBL2113242 1 4.68
CHEMBL213137 1 -
CHEMBL211575 1 -
CHEMBL2113241 1 -
CHEMBL2113240 1 -
CHEMBL2113239 1 -
CHEMBL2113238 1 -
CHEMBL2113233 1 -
CHEMBL2113232 1 -
CHEMBL2113228 1 -
CHEMBL2113236 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192704 IC50 = 2000.0 nM 5.70
CHEMBL213024 IC50 = 9000.0 nM 5.05
CHEMBL2113242 IC50 = 21000.0 nM 4.68
CHEMBL213137 IC50 > 30000.0 nM -
CHEMBL211575 IC50 > 30000.0 nM -
CHEMBL2113241 IC50 > 30000.0 nM -
CHEMBL2113240 IC50 > 30000.0 nM -
CHEMBL2113239 IC50 > 30000.0 nM -
CHEMBL2113238 IC50 > 30000.0 nM -
CHEMBL2113233 IC50 > 30000.0 nM -
CHEMBL2113232 IC50 > 30000.0 nM -
CHEMBL2113228 IC50 > 30000.0 nM -
CHEMBL2113236 IC50 > 30000.0 nM -