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Assay Detail

CHEMBL670592

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

Functional
Inhibition of [3H]dopamine uptake at the dopamine transporter in rat striatal tissue
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Striatum
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
Houlihan WJ, Boja JW, Parrino VA, Kopajtic TA, Kuhar MJ.
J Med Chem (1996) 39 : 4935 -4941
PubMed 8960553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.88 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337510 1 9.59
CHEMBL133786 1 8.89
CHEMBL129899 1 8.85
CHEMBL130477 1 8.85
CHEMBL130394 1 8.77
CHEMBL133795 1 8.51
CHEMBL130255 1 8.47
CHEMBL781 MAZINDOL 4.0 1 8.08
CHEMBL336654 1 8.07
CHEMBL132198 1 8.07
CHEMBL132241 1 8.04
CHEMBL129885 1 7.96
CHEMBL335296 1 7.85
CHEMBL336413 1 7.82
CHEMBL337052 1 7.75
CHEMBL133355 1 7.59
CHEMBL339169 1 7.28
CHEMBL336313 1 7.26
CHEMBL442765 1 7.24
CHEMBL147748 1 7.11
CHEMBL132206 1 7.05
CHEMBL130198 1 7.04
CHEMBL133902 1 6.91
CHEMBL339841 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337510 IC50 = 0.26 nM 9.59
CHEMBL133786 IC50 = 1.3 nM 8.89
CHEMBL129899 IC50 = 1.4 nM 8.85
CHEMBL130477 IC50 = 1.4 nM 8.85
CHEMBL130394 IC50 = 1.7 nM 8.77
CHEMBL133795 IC50 = 3.1 nM 8.51
CHEMBL130255 IC50 = 3.4 nM 8.47
CHEMBL781 MAZINDOL IC50 = 8.4 nM 8.08
CHEMBL336654 IC50 = 8.5 nM 8.07
CHEMBL132198 IC50 = 8.6 nM 8.07
CHEMBL132241 IC50 = 9.2 nM 8.04
CHEMBL129885 IC50 = 11.0 nM 7.96
CHEMBL335296 IC50 = 14.0 nM 7.85
CHEMBL336413 IC50 = 15.0 nM 7.82
CHEMBL337052 IC50 = 18.0 nM 7.75
CHEMBL133355 IC50 = 25.4 nM 7.59
CHEMBL339169 IC50 = 53.0 nM 7.28
CHEMBL336313 IC50 = 55.0 nM 7.26
CHEMBL442765 IC50 = 58.0 nM 7.24
CHEMBL147748 IC50 = 78.0 nM 7.11
CHEMBL132206 IC50 = 89.0 nM 7.05
CHEMBL130198 IC50 = 92.0 nM 7.04
CHEMBL133902 IC50 = 124.0 nM 6.91
CHEMBL339841 IC50 = 770.0 nM 6.11