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Assay Detail

CHEMBL671638

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

Binding
Inhibition of [3H]WIN-35428 binding to rat striatal membrane dopamine transporter
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and ligand binding of cocaine isomers at the cocaine receptor.
Carroll FI, Lewin AH, Abraham P, Parham K, Boja JW, Kuhar MJ.
J Med Chem (1991) 34 : 883 -886
PubMed 2002468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.02 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 2 6.99
CHEMBL352487 2 5.21
CHEMBL170745 1 5.01
CHEMBL352575 1 4.80
CHEMBL171007 1 4.65
CHEMBL171201 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE IC50 = 102.0 nM 6.99
CHEMBL352487 IC50 = 6160.0 nM 5.21
CHEMBL170745 IC50 = 9820.0 nM 5.01
CHEMBL370805 COCAINE IC50 = 15800.0 nM 4.80
CHEMBL352575 IC50 = 15800.0 nM 4.80
CHEMBL171007 IC50 = 22500.0 nM 4.65
CHEMBL352487 IC50 = 28500.0 nM 4.54
CHEMBL171201 IC50 = 67700.0 nM 4.17