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Assay Detail

CHEMBL4219684

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Binding
Binding affinity to human DAT
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.
Subbaiah MAM.
J Med Chem (2018) 61 : 2133 -2165
PubMed 28731336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.74 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228464 1 8.82
CHEMBL4227100 1 8.30
CHEMBL4227688 1 8.24
CHEMBL1173532 GSK1360707 1.0 1 8.00
CHEMBL4224830 3 7.90
CHEMBL4227955 1 7.40
CHEMBL4227027 1 7.40
CHEMBL4226867 1 7.10
CHEMBL4225921 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228464 Ki = 1.514 nM 8.82
CHEMBL4227100 Ki = 5.012 nM 8.30
CHEMBL4227688 Ki = 5.754 nM 8.24
CHEMBL1173532 GSK1360707 Ki = 10.0 nM 8.00
CHEMBL4224830 Ki = 12.59 nM 7.90
CHEMBL4224830 Ki = 19.95 nM 7.70
CHEMBL4224830 Ki = 31.62 nM 7.50
CHEMBL4227955 Ki = 39.81 nM 7.40
CHEMBL4227027 Ki = 39.81 nM 7.40
CHEMBL4226867 Ki = 79.43 nM 7.10
CHEMBL4225921 Ki = 158.49 nM 6.80