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Assay Detail

CHEMBL915412

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

Binding
Displacement of [3H]WIN-35428 from DAT
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Carroll FI, Runyon SP, Abraham P, Navarro H, Kuhar MJ, Pollard GT, Howard JL.
J Med Chem (2004) 47 : 6401 -6409
PubMed 15566309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.83 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610897 1 8.96
CHEMBL311347 1 8.89
CHEMBL218082 1 8.77
CHEMBL224819 1 8.77
CHEMBL312037 1 8.77
CHEMBL375889 1 8.54
CHEMBL375888 1 8.51
CHEMBL373385 1 7.99
CHEMBL374712 1 7.93
CHEMBL2079586 1 7.86
CHEMBL2096859 1 7.80
CHEMBL222705 1 7.68
CHEMBL83729 1 7.64
CHEMBL2096860 1 7.64
CHEMBL221993 1 7.63
CHEMBL2096858 1 7.60
CHEMBL370805 COCAINE 4.0 1 7.05
CHEMBL376899 1 7.00
CHEMBL2096861 1 6.68
CHEMBL2096857 1 6.49
CHEMBL2096856 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610897 IC50 = 1.1 nM 8.96
CHEMBL311347 IC50 = 1.3 nM 8.89
CHEMBL218082 IC50 = 1.7 nM 8.77
CHEMBL224819 IC50 = 1.7 nM 8.77
CHEMBL312037 IC50 = 1.7 nM 8.77
CHEMBL375889 IC50 = 2.9 nM 8.54
CHEMBL375888 IC50 = 3.1 nM 8.51
CHEMBL373385 IC50 = 10.2 nM 7.99
CHEMBL374712 IC50 = 11.7 nM 7.93
CHEMBL2079586 IC50 = 13.9 nM 7.86
CHEMBL2096859 IC50 = 15.7 nM 7.80
CHEMBL222705 IC50 = 21.0 nM 7.68
CHEMBL83729 IC50 = 23.0 nM 7.64
CHEMBL2096860 IC50 = 22.7 nM 7.64
CHEMBL221993 IC50 = 23.4 nM 7.63
CHEMBL2096858 IC50 = 25.0 nM 7.60
CHEMBL370805 COCAINE IC50 = 89.1 nM 7.05
CHEMBL376899 IC50 = 101.0 nM 7.00
CHEMBL2096861 IC50 = 207.0 nM 6.68
CHEMBL2096857 IC50 = 325.0 nM 6.49
CHEMBL2096856 IC50 = 670.0 nM 6.17