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Assay Detail

CHEMBL670825

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

Binding
Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Tolerance in the replacement of the benzhydrylic O atom in 4-[2-(diphenylmethoxy)ethyl]-1-benzylpiperidine derivatives by an N atom: development of new-generation potent and selective N-analogue molecules for the dopamine transporter.
Dutta AK, Xu C, Reith ME.
J Med Chem (1998) 41 : 3293 -3297
PubMed 9703474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.12 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110530 1 7.52
CHEMBL444592 1 7.48
CHEMBL34032 1 7.46
CHEMBL20648 1 7.42
CHEMBL281594 VANOXERINE 3.0 1 7.37
CHEMBL109776 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110530 IC50 = 30.0 nM 7.52
CHEMBL444592 IC50 = 33.0 nM 7.48
CHEMBL34032 IC50 = 35.0 nM 7.46
CHEMBL20648 IC50 = 37.6 nM 7.42
CHEMBL281594 VANOXERINE IC50 = 43.0 nM 7.37
CHEMBL109776 IC50 = 3213.0 nM 5.49