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Assay Detail

CHEMBL674113

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

Binding
Inhibition of [3H]dopamine uptake at dopamine transporter.
12
Total Activities
7
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 12 6.05 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL177269 1 7.11
CHEMBL369375 1 6.66
CHEMBL352575 4 6.50
CHEMBL174568 1 6.10
CHEMBL120901 3 6.06
CHEMBL369016 1 5.85
CHEMBL3143431 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL177269 IC50 = 77.0 nM 7.11
CHEMBL369375 IC50 = 220.0 nM 6.66
CHEMBL352575 IC50 = 317.0 nM 6.50
CHEMBL352575 IC50 = 690.0 nM 6.16
CHEMBL174568 IC50 = 800.0 nM 6.10
CHEMBL352575 IC50 = 815.0 nM 6.09
CHEMBL120901 IC50 = 870.0 nM 6.06
CHEMBL369016 IC50 = 1400.0 nM 5.85
CHEMBL352575 IC50 = 2420.0 nM 5.62
CHEMBL3143431 IC50 = 2480.0 nM 5.61
CHEMBL120901 IC50 = 2750.0 nM 5.56
CHEMBL120901 IC50 = 5020.0 nM 5.30