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Assay Detail

CHEMBL4219686

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

Binding
Binding affinity to human NET
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 noradrenaline transporter (CHEMBL222)
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 8.05 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4228464 1 10.10
CHEMBL4227688 1 8.85
CHEMBL4227100 1 8.50
CHEMBL4224830 3 8.40
CHEMBL4226867 1 8.20
CHEMBL1173532 GSK1360707 1.0 1 8.10
CHEMBL4227027 1 7.30
CHEMBL4227955 1 7.10
CHEMBL4225921 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4228464 Ki = 0.07943 nM 10.10
CHEMBL4227688 Ki = 1.413 nM 8.85
CHEMBL4227100 Ki = 3.162 nM 8.50
CHEMBL4224830 Ki = 3.981 nM 8.40
CHEMBL4226867 Ki = 6.31 nM 8.20
CHEMBL1173532 GSK1360707 Ki = 7.943 nM 8.10
CHEMBL4224830 Ki = 10.0 nM 8.00
CHEMBL4227027 Ki = 50.12 nM 7.30
CHEMBL4224830 Ki = 63.1 nM 7.20
CHEMBL4227955 Ki = 79.43 nM 7.10
CHEMBL4225921 Ki = 158.49 nM 6.80