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Assay Detail

CHEMBL678245

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Binding
Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Caudate-putamen
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and dopamine transporter binding affinities of 3alpha-benzyl-8-(diarylmethoxyethyl)-8-azabicyclo[3.2.1]octanes.
Bradley AL, Izenwasser S, Wade D, Klein-Stevens C, Zhu N, Trudell ML.
Bioorg Med Chem Lett (2002) 12 : 2387 -2390
PubMed 12161139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.91 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 7.92
CHEMBL77867 1 7.60
CHEMBL306314 1 7.01
CHEMBL76603 1 7.00
CHEMBL80245 1 6.87
CHEMBL79490 1 6.84
CHEMBL370805 COCAINE 4.0 1 6.73
CHEMBL311044 1 6.70
CHEMBL306528 1 6.66
CHEMBL306359 1 6.46
CHEMBL433138 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE Ki = 12.0 nM 7.92
CHEMBL77867 Ki = 25.0 nM 7.60
CHEMBL306314 Ki = 98.0 nM 7.01
CHEMBL76603 Ki = 99.0 nM 7.00
CHEMBL80245 Ki = 135.0 nM 6.87
CHEMBL79490 Ki = 144.0 nM 6.84
CHEMBL370805 COCAINE Ki = 187.0 nM 6.73
CHEMBL311044 Ki = 198.0 nM 6.70
CHEMBL306528 Ki = 217.0 nM 6.66
CHEMBL306359 Ki = 346.0 nM 6.46
CHEMBL433138 Ki = 595.0 nM 6.22