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Assay Detail

CHEMBL847532

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

Binding
Inhibition of [3H]paroxetine binding to serotonin transporter (SERT) of rat cortical membrane
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Substituted diphenyl sulfides as selective serotonin transporter ligands: synthesis and in vitro evaluation.
Emond P, Vercouillie J, Innis R, Chalon S, Mavel S, Frangin Y, Halldin C, Besnard JC, Guilloteau D.
J Med Chem (2002) 45 : 1253 -1258
PubMed 11881994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.36 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23034 1 9.40
CHEMBL429065 1 9.01
CHEMBL278809 1 8.90
CHEMBL23033 1 8.83
CHEMBL22183 1 8.78
CHEMBL278165 1 8.72
CHEMBL22216 1 8.65
CHEMBL284002 1 8.60
CHEMBL22259 1 8.56
CHEMBL22743 1 8.10
CHEMBL22643 1 7.71
CHEMBL277045 1 7.27
CHEMBL22436 1 6.16
CHEMBL441022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23034 Ki = 0.4 nM 9.40
CHEMBL429065 Ki = 0.98 nM 9.01
CHEMBL278809 Ki = 1.25 nM 8.90
CHEMBL23033 Ki = 1.49 nM 8.83
CHEMBL22183 Ki = 1.65 nM 8.78
CHEMBL278165 Ki = 1.92 nM 8.72
CHEMBL22216 Ki = 2.23 nM 8.65
CHEMBL284002 Ki = 2.5 nM 8.60
CHEMBL22259 Ki = 2.75 nM 8.56
CHEMBL22743 Ki = 7.96 nM 8.10
CHEMBL22643 Ki = 19.3 nM 7.71
CHEMBL277045 Ki = 53.3 nM 7.27
CHEMBL22436 Ki = 695.0 nM 6.16
CHEMBL441022 Ki > 1000.0 nM -