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Assay Detail

CHEMBL830133

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

Binding
In vitro inhibition of [3H]citalopram binding to human serotonin transporter expressed in human HEK293 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
Jarkas N, McConathy J, Voll RJ, Goodman MM.
J Med Chem (2005) 48 : 4254 -4265
PubMed 15974579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.54 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23034 1 10.89
CHEMBL22183 1 9.60
CHEMBL189367 1 9.31
CHEMBL190937 1 9.24
CHEMBL190703 1 8.95
CHEMBL190700 1 8.80
CHEMBL2113054 1 8.71
CHEMBL189375 1 8.69
CHEMBL188964 1 8.07
CHEMBL363396 1 8.07
CHEMBL362783 1 7.82
CHEMBL187935 1 7.30
CHEMBL2113055 1 7.08
CHEMBL413562 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23034 Ki = 0.013 nM 10.89
CHEMBL22183 Ki = 0.25 nM 9.60
CHEMBL189367 Ki = 0.49 nM 9.31
CHEMBL190937 Ki = 0.57 nM 9.24
CHEMBL190703 Ki = 1.12 nM 8.95
CHEMBL190700 Ki = 1.59 nM 8.80
CHEMBL2113054 Ki = 1.94 nM 8.71
CHEMBL189375 Ki = 2.04 nM 8.69
CHEMBL188964 Ki = 8.5 nM 8.07
CHEMBL363396 Ki = 8.55 nM 8.07
CHEMBL362783 Ki = 15.11 nM 7.82
CHEMBL187935 Ki = 50.58 nM 7.30
CHEMBL2113055 Ki = 83.43 nM 7.08
CHEMBL413562 Ki = 92.26 nM 7.04