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Assay Detail

CHEMBL679182

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Binding
The compound has been evaluated for its binding affinity towards Dopamine transporter by displacing the radioligand [3H]GBR-12935 (1.0 nM) in rat striatal synaptosomes.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.
Kawai H, Kotake Y, Ohta S.
Bioorg Med Chem Lett (2000) 10 : 1669 -1671
PubMed 10937721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 4.45 4.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL44877 1 4.67
CHEMBL21640 1 4.44
CHEMBL298285 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL44877 Ki = 21490.0 nM 4.67
CHEMBL21640 Ki = 36620.0 nM 4.44
CHEMBL298285 Ki = 57550.0 nM 4.24