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Assay Detail

CHEMBL674120

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

Binding
Displacement of [3H]mazindol from dopamine transporter
10
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 (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency
Kozikowski AP, Roberti M, Johnson KM, Bergmann JS, Ball RG
Bioorg Med Chem Lett (1993) 3 : 1327 -1332
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.54 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28394 2 9.44
CHEMBL27336 1 8.46
CHEMBL27586 1 8.04
CHEMBL2115570 2 7.75
CHEMBL285342 2 6.78
CHEMBL120901 1 6.31
CHEMBL28376 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28394 IC50 = 0.36 nM 9.44
CHEMBL28394 IC50 = 0.73 nM 9.14
CHEMBL27336 IC50 = 3.5 nM 8.46
CHEMBL27586 IC50 = 9.2 nM 8.04
CHEMBL2115570 IC50 = 18.0 nM 7.75
CHEMBL2115570 IC50 = 24.0 nM 7.62
CHEMBL285342 IC50 = 166.0 nM 6.78
CHEMBL120901 IC50 = 490.0 nM 6.31
CHEMBL285342 IC50 = 1105.0 nM 5.96
CHEMBL28376 IC50 = 1190.0 nM 5.92