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Assay Detail

CHEMBL805339

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Binding
Binding affinity towards serotonin transporter using [3H]citalopram as radioligand was determined
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.
Zou MF, Kopajtic T, Katz JL, Newman AH.
J Med Chem (2003) 46 : 2908 -2916
PubMed 12825932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.02 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42553 1 8.84
CHEMBL310650 1 6.16
CHEMBL98279 1 5.82
CHEMBL317362 1 5.73
CHEMBL316634 1 5.69
CHEMBL95775 1 5.50
CHEMBL317757 DIFLUOROBENZTROPINE 1 5.49
CHEMBL99038 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42553 Ki = 1.46 nM 8.84
CHEMBL310650 Ki = 690.0 nM 6.16
CHEMBL98279 Ki = 1500.0 nM 5.82
CHEMBL317362 Ki = 1850.0 nM 5.73
CHEMBL316634 Ki = 2040.0 nM 5.69
CHEMBL95775 Ki = 3160.0 nM 5.50
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 3260.0 nM 5.49
CHEMBL99038 Ki = 12000.0 nM 4.92