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Assay Detail

CHEMBL809435

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Binding
Compound was tested for the inhibition of serotonin [3H]SER reuptake into rat forebrain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Forebrain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Discovery of substituted 3,4-diphenyl-thiazoles as a novel class of monoamine transporter inhibitors through 3-D pharmacophore search using a new pharmacophore model derived from mazindol.
Enyedy IJ, Wang J, Zaman WA, Johnson KM, Wang S.
Bioorg Med Chem Lett (2002) 12 : 1775 -1778
PubMed 12067559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.36 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL297102 1 7.17
CHEMBL120901 1 6.81
CHEMBL48892 1 6.65
CHEMBL296907 1 6.40
CHEMBL50901 1 6.37
CHEMBL301094 1 6.36
CHEMBL52392 1 6.07
CHEMBL49736 1 5.85
CHEMBL51993 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL297102 Ki = 67.0 nM 7.17
CHEMBL120901 Ki = 155.0 nM 6.81
CHEMBL48892 Ki = 225.0 nM 6.65
CHEMBL296907 Ki = 398.0 nM 6.40
CHEMBL50901 Ki = 424.0 nM 6.37
CHEMBL301094 Ki = 433.0 nM 6.36
CHEMBL52392 Ki = 843.0 nM 6.07
CHEMBL49736 Ki = 1410.0 nM 5.85
CHEMBL51993 Ki = 2617.0 nM 5.58