Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL670828

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

Binding
Inhibition of [3H]dopamine reuptake in HEK293 cells expressing human dopamine transporter
12
Total Activities
12
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 Expert

Target

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

Publication

Novel 3-aminomethyl- and 4-aminopiperidine analogues of 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazines: synthesis and evaluation as dopamine transporter ligands.
Choi SW, Elmaleh DR, Hanson RN, Fischman AJ.
J Med Chem (2000) 43 : 205 -213
PubMed 10649976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.63 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26320 1 7.75
CHEMBL67078 1 6.98
CHEMBL67203 1 6.82
CHEMBL370805 COCAINE 4.0 1 6.72
CHEMBL443797 1 6.68
CHEMBL63703 1 6.57
CHEMBL67024 1 6.50
CHEMBL417049 1 6.48
CHEMBL417035 1 6.44
CHEMBL421867 1 6.41
CHEMBL66112 1 6.30
CHEMBL69380 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26320 IC50 = 18.0 nM 7.75
CHEMBL67078 IC50 = 105.0 nM 6.98
CHEMBL67203 IC50 = 150.0 nM 6.82
CHEMBL370805 COCAINE IC50 = 190.0 nM 6.72
CHEMBL443797 IC50 = 210.0 nM 6.68
CHEMBL63703 IC50 = 270.0 nM 6.57
CHEMBL67024 IC50 = 320.0 nM 6.50
CHEMBL417049 IC50 = 330.0 nM 6.48
CHEMBL417035 IC50 = 364.0 nM 6.44
CHEMBL421867 IC50 = 390.0 nM 6.41
CHEMBL66112 IC50 = 500.0 nM 6.30
CHEMBL69380 IC50 = 1260.0 nM 5.90