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Assay Detail

CHEMBL1023032

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

Binding
Displacement of [125I]RTI-55 from human recombinant DAT expressed in HEK293 cells by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.
Cashman JR, Voelker T, Zhang HT, O'Donnell JM.
J Med Chem (2009) 52 : 1530 -1539
PubMed 19256502 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.28 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 1 6.43
CHEMBL505431 1 5.61
CHEMBL451500 1 5.27
CHEMBL464422 1 5.19
CHEMBL41 FLUOXETINE 4.0 1 5.18
CHEMBL450907 1 5.14
CHEMBL473966 1 4.17
CHEMBL313041 1 -
CHEMBL463431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE Ki = 371.0 nM 6.43
CHEMBL505431 Ki = 2478.0 nM 5.61
CHEMBL451500 Ki = 5340.0 nM 5.27
CHEMBL464422 Ki = 6500.0 nM 5.19
CHEMBL41 FLUOXETINE Ki = 6670.0 nM 5.18
CHEMBL450907 Ki = 7307.0 nM 5.14
CHEMBL473966 Ki = 66988.0 nM 4.17
CHEMBL313041 Ki > 100000.0 nM -
CHEMBL463431 Ki > 100000.0 nM -