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Assay Detail

CHEMBL4202148

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

Binding
Displacement of [125I]RTI-55 from human DAT expressed in HEK293 cell membranes
13
Total Activities
12
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

Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter.
Provencher BA, Eshleman AJ, Johnson RA, Shi X, Kryatova O, Nelson J, Tian J, Gonzalez M, Meltzer PC, Janowsky A.
J Med Chem (2018) 61 : 9121 -9131
PubMed 30240563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.38 5.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4207658 1 5.79
CHEMBL4205254 2 5.61
CHEMBL4202787 1 5.38
CHEMBL4216117 1 5.14
CHEMBL4214975 1 -
CHEMBL4203894 1 -
CHEMBL4208779 1 -
CHEMBL4204449 1 -
CHEMBL4212633 1 -
CHEMBL4217581 1 -
CHEMBL4208250 1 -
CHEMBL4213176 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4207658 Ki = 1610.0 nM 5.79
CHEMBL4205254 Ki = 2440.0 nM 5.61
CHEMBL4202787 Ki = 4170.0 nM 5.38
CHEMBL4216117 Ki = 7300.0 nM 5.14
CHEMBL4205254 Ki = 9900.0 nM 5.00
CHEMBL4214975 Ki > 9300.0 nM -
CHEMBL4203894 Ki > 10000.0 nM -
CHEMBL4208779 Ki > 10000.0 nM -
CHEMBL4204449 Ki > 10000.0 nM -
CHEMBL4212633 Ki > 10000.0 nM -
CHEMBL4217581 Ki > 10000.0 nM -
CHEMBL4208250 Ki > 7100.0 nM -
CHEMBL4213176 Ki > 10000.0 nM -