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Assay Detail

CHEMBL2215837

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

Binding
Inhibition of DAT-mediated [3H]DA in rat synaptosomes by scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB.
J Med Chem (2011) 54 : 3206 -3221
PubMed 21486038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.86 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204356 1 7.68
CHEMBL2205043 1 7.43
CHEMBL2205045 1 6.96
CHEMBL2205054 1 6.92
CHEMBL2204357 1 6.77
CHEMBL2204359 1 6.60
CHEMBL2204363 1 6.50
CHEMBL2204360 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204356 IC50 = 21.0 nM 7.68
CHEMBL2205043 IC50 = 37.0 nM 7.43
CHEMBL2205045 IC50 = 110.0 nM 6.96
CHEMBL2205054 IC50 = 120.0 nM 6.92
CHEMBL2204357 IC50 = 170.0 nM 6.77
CHEMBL2204359 IC50 = 250.0 nM 6.60
CHEMBL2204363 IC50 = 320.0 nM 6.50
CHEMBL2204360 IC50 = 890.0 nM 6.05