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Assay Detail

CHEMBL809432

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

Binding
Ability to displace [3H]citalopram radioligand, for the Serotonin transporter in rat brain
9
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
Zou MF, Agoston GE, Belov Y, Kopajtic T, Katz JL, Newman AH.
Bioorg Med Chem Lett (2002) 12 : 1249 -1252
PubMed 11965364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.50 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21859 2 6.16
CHEMBL281388 2 5.73
CHEMBL283154 2 5.69
CHEMBL317757 DIFLUOROBENZTROPINE 1 5.49
CHEMBL428704 2 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21859 Ki = 690.0 nM 6.16
CHEMBL21859 Ki = 1750.0 nM 5.76
CHEMBL281388 Ki = 1850.0 nM 5.73
CHEMBL283154 Ki = 2040.0 nM 5.69
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 3260.0 nM 5.49
CHEMBL283154 Ki = 3320.0 nM 5.48
CHEMBL281388 Ki = 3740.0 nM 5.43
CHEMBL428704 Ki = 12000.0 nM 4.92
CHEMBL428704 Ki = 13800.0 nM 4.86