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Assay Detail

CHEMBL678931

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

Binding
Binding affinity at Dopamine transporter by displacing [3H]WIN-35428 from rat caudate putamen
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

[3-cis-3,5-Dimethyl-(1-piperazinyl)alkyl]-bis-(4'-fluorophenyl)amine analogues as novel probes for the dopamine transporter.
Cao J, Husbands SM, Kopajtic T, Katz JL, Newman AH.
Bioorg Med Chem Lett (2001) 11 : 3169 -3173
PubMed 11720867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.02 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 7.92
CHEMBL313179 1 7.75
CHEMBL316244 1 7.21
CHEMBL433340 1 7.08
CHEMBL86830 1 6.88
CHEMBL275707 RIMCAZOLE 2.0 1 6.65
CHEMBL84971 1 6.58
CHEMBL314433 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE Ki = 11.9 nM 7.92
CHEMBL313179 Ki = 17.6 nM 7.75
CHEMBL316244 Ki = 61.0 nM 7.21
CHEMBL433340 Ki = 83.2 nM 7.08
CHEMBL86830 Ki = 131.0 nM 6.88
CHEMBL275707 RIMCAZOLE Ki = 224.0 nM 6.65
CHEMBL84971 Ki = 261.0 nM 6.58
CHEMBL314433 Ki = 813.0 nM 6.09