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Assay Detail

CHEMBL884454

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

Binding
Inhibition of [3H]dopamine uptake at dopamine transporter.
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
Carroll FI, Lewin AH, Boja JW, Kuhar MJ.
J Med Chem (1992) 35 : 969 -981
PubMed 1552510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.99 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2079586 1 7.10
CHEMBL2373962 1 6.96
CHEMBL159325 1 6.75
CHEMBL1790051 3 6.02
CHEMBL172482 1 5.60
CHEMBL425862 1 5.60
CHEMBL426954 1 5.56
CHEMBL120901 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2079586 IC50 = 80.0 nM 7.10
CHEMBL2373962 IC50 = 110.0 nM 6.96
CHEMBL159325 IC50 = 178.0 nM 6.75
CHEMBL1790051 IC50 = 960.0 nM 6.02
CHEMBL1790051 IC50 = 1330.0 nM 5.88
CHEMBL172482 IC50 = 2500.0 nM 5.60
CHEMBL425862 IC50 = 2500.0 nM 5.60
CHEMBL426954 IC50 = 2780.0 nM 5.56
CHEMBL120901 IC50 = 36000.0 nM 4.44
CHEMBL1790051 IC50 = 200000.0 nM -