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Assay Detail

CHEMBL3128346

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

Binding
Binding affinity to human SERT T497A mutant expressed in African green monkey COS7 cells assessed as inhibition of [3H]-serotonin uptake after 3 mins by beta-scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.
Okunola-Bakare OM, Cao J, Kopajtic T, Katz JL, Loland CJ, Shi L, Newman AH.
J Med Chem (2014) 57 : 1000 -1013
PubMed 24494745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.85 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3126730 1 6.77
CHEMBL1516187 1 6.20
CHEMBL3126751 1 4.57
CHEMBL1373 MODAFINIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3126730 Ki = 170.0 nM 6.77
CHEMBL1516187 Ki = 630.0 nM 6.20
CHEMBL3126751 Ki = 27000.0 nM 4.57
CHEMBL1373 MODAFINIL Ki = 570000.0 nM -