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Assay Detail

CHEMBL672590

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

Binding
Ability to displace [3H]WIN-35428 from Dopamine Transporter of rat striatal membrane
24
Total Activities
24
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

Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Houlihan WJ, Kelly L, Pankuch J, Koletar J, Brand L, Janowsky A, Kopajtic TA.
J Med Chem (2002) 45 : 4097 -4109
PubMed 12213053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.02 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130477 1 9.00
CHEMBL544370 1 8.71
CHEMBL133043 1 8.60
CHEMBL130668 1 8.47
CHEMBL781 MAZINDOL 4.0 1 8.09
CHEMBL132955 1 7.87
CHEMBL442765 1 7.24
CHEMBL336761 1 7.20
CHEMBL133902 1 7.18
CHEMBL338721 1 7.15
CHEMBL130372 1 7.06
CHEMBL336313 1 7.06
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL339648 1 7.03
CHEMBL424640 1 7.00
CHEMBL555778 1 6.66
CHEMBL133287 1 6.64
CHEMBL131637 1 6.54
CHEMBL130747 1 6.20
CHEMBL134129 1 6.00
CHEMBL132180 1 5.56
CHEMBL132419 1 5.48
CHEMBL132988 1 5.43
CHEMBL336624 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130477 IC50 = 1.0 nM 9.00
CHEMBL544370 IC50 = 1.94 nM 8.71
CHEMBL133043 IC50 = 2.5 nM 8.60
CHEMBL130668 IC50 = 3.4 nM 8.47
CHEMBL781 MAZINDOL IC50 = 8.1 nM 8.09
CHEMBL132955 IC50 = 13.6 nM 7.87
CHEMBL442765 IC50 = 57.1 nM 7.24
CHEMBL336761 IC50 = 62.5 nM 7.20
CHEMBL133902 IC50 = 66.0 nM 7.18
CHEMBL338721 IC50 = 71.5 nM 7.15
CHEMBL130372 IC50 = 87.4 nM 7.06
CHEMBL336313 IC50 = 86.4 nM 7.06
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL339648 IC50 = 93.3 nM 7.03
CHEMBL424640 IC50 = 99.8 nM 7.00
CHEMBL555778 IC50 = 219.0 nM 6.66
CHEMBL133287 IC50 = 230.0 nM 6.64
CHEMBL131637 IC50 = 290.0 nM 6.54
CHEMBL130747 IC50 = 638.0 nM 6.20
CHEMBL134129 IC50 = 1009.0 nM 6.00
CHEMBL132180 IC50 = 2770.0 nM 5.56
CHEMBL132419 IC50 = 3310.0 nM 5.48
CHEMBL132988 IC50 = 3700.0 nM 5.43
CHEMBL336624 IC50 = 6890.0 nM 5.16