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Assay Detail

CHEMBL4276207

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

Binding
Inhibition of [3H]dopamine uptake at human DAT expressed in HEK293 cells after 15 to 20 mins by microbeta scintillation counting method
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.
Paudel S, Min X, Acharya S, Khadka DB, Yoon G, Kim KM, Cheon SH.
Bioorg Med Chem (2018) 26 : 5538 -5546
PubMed 30293797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.05 6.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4288240 1 6.09
CHEMBL4082902 1 6.01
CHEMBL4245867 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4288240 IC50 = 820.0 nM 6.09
CHEMBL4082902 IC50 = 980.0 nM 6.01
CHEMBL4245867 IC50 > 10000.0 nM -