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Assay Detail

CHEMBL672120

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

Binding
Ability to displace [3H]WIN-35428 from dopamine transporter in rat caudate putamen tissue
71
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Caudate-putamen
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.
Kulkarni SS, Newman AH, Houlihan WJ.
J Med Chem (2002) 45 : 4119 -4127
PubMed 12213055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 71 6.84 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130477 1 9.00
CHEMBL133786 1 9.00
CHEMBL130255 1 8.82
CHEMBL337510 1 8.77
CHEMBL133795 1 8.70
CHEMBL133043 1 8.60
CHEMBL129899 1 8.60
CHEMBL132198 1 8.59
CHEMBL336654 1 8.49
CHEMBL130668 1 8.47
CHEMBL132241 1 8.37
CHEMBL337052 1 8.24
CHEMBL129885 1 8.23
CHEMBL130394 1 8.20
CHEMBL336413 1 8.19
CHEMBL781 MAZINDOL 4.0 1 8.09
CHEMBL335318 1 8.00
CHEMBL133355 1 7.89
CHEMBL132955 1 7.85
CHEMBL133646 1 7.80
CHEMBL335296 1 7.77
CHEMBL132676 1 7.64
CHEMBL132206 1 7.64
CHEMBL334535 1 7.47
CHEMBL334577 1 7.43
CHEMBL340281 1 7.42
CHEMBL134098 1 7.38
CHEMBL337299 1 7.30
CHEMBL339169 1 7.28
CHEMBL442765 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133786 IC50 = 1.0 nM 9.00
CHEMBL130477 IC50 = 1.0 nM 9.00
CHEMBL130255 IC50 = 1.5 nM 8.82
CHEMBL337510 IC50 = 1.7 nM 8.77
CHEMBL133795 IC50 = 2.0 nM 8.70
CHEMBL133043 IC50 = 2.5 nM 8.60
CHEMBL129899 IC50 = 2.5 nM 8.60
CHEMBL132198 IC50 = 2.6 nM 8.59
CHEMBL336654 IC50 = 3.2 nM 8.49
CHEMBL130668 IC50 = 3.4 nM 8.47
CHEMBL132241 IC50 = 4.3 nM 8.37
CHEMBL337052 IC50 = 5.8 nM 8.24
CHEMBL129885 IC50 = 5.9 nM 8.23
CHEMBL130394 IC50 = 6.3 nM 8.20
CHEMBL336413 IC50 = 6.5 nM 8.19
CHEMBL781 MAZINDOL IC50 = 8.1 nM 8.09
CHEMBL335318 IC50 = 10.0 nM 8.00
CHEMBL133355 IC50 = 13.0 nM 7.89
CHEMBL132955 IC50 = 14.0 nM 7.85
CHEMBL133646 IC50 = 16.0 nM 7.80
CHEMBL335296 IC50 = 17.0 nM 7.77
CHEMBL132676 IC50 = 23.0 nM 7.64
CHEMBL132206 IC50 = 23.0 nM 7.64
CHEMBL334535 IC50 = 34.0 nM 7.47
CHEMBL334577 IC50 = 37.0 nM 7.43
CHEMBL340281 IC50 = 38.0 nM 7.42
CHEMBL134098 IC50 = 42.0 nM 7.38
CHEMBL337299 IC50 = 50.0 nM 7.30
CHEMBL339169 IC50 = 53.0 nM 7.28
CHEMBL442765 IC50 = 57.0 nM 7.24
CHEMBL336761 IC50 = 63.0 nM 7.20
CHEMBL133902 IC50 = 66.0 nM 7.18
CHEMBL338721 IC50 = 72.0 nM 7.14
CHEMBL130198 IC50 = 77.0 nM 7.11
CHEMBL336313 IC50 = 86.0 nM 7.07
CHEMBL130372 IC50 = 87.0 nM 7.06
CHEMBL339648 IC50 = 93.0 nM 7.03
CHEMBL424640 IC50 = 100.0 nM 7.00
CHEMBL134218 IC50 = 190.0 nM 6.72
CHEMBL337468 IC50 = 190.0 nM 6.72
CHEMBL133287 IC50 = 230.0 nM 6.64
CHEMBL339841 IC50 = 290.0 nM 6.54
CHEMBL131637 IC50 = 290.0 nM 6.54
CHEMBL132630 IC50 = 320.0 nM 6.50
CHEMBL336547 IC50 = 560.0 nM 6.25
CHEMBL130747 IC50 = 640.0 nM 6.19
CHEMBL340392 IC50 = 720.0 nM 6.14
CHEMBL129962 IC50 = 1200.0 nM 5.92
CHEMBL337634 IC50 = 1300.0 nM 5.89
CHEMBL337004 IC50 = 1600.0 nM 5.80