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Assay Detail

CHEMBL872897

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

Binding
Affinity for dopamine transporter was assessed by the ability to displace [3H]WIN-35428 from rat caudate-putamen tissue
9
Total Activities
9
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

Synthesis and biological evaluation of 2-substituted 3beta-tolyltropane derivatives at dopamine, serotonin, and norepinephrine transporters.
Xu L, Izenwasser S, Katz JL, Kopajtic T, Klein-Stevens C, Zhu N, Lomenzo SA, Winfield L, Trudell ML.
J Med Chem (2002) 45 : 1203 -1210
PubMed 11881989 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.22 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19944 1 7.96
CHEMBL2079577 1 7.85
CHEMBL279074 1 7.77
CHEMBL2079656 1 7.60
CHEMBL370805 COCAINE 4.0 1 7.50
CHEMBL2112763 1 7.07
CHEMBL276332 1 6.91
CHEMBL19715 1 6.87
CHEMBL2112762 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19944 Ki = 11.0 nM 7.96
CHEMBL2079577 Ki = 14.0 nM 7.85
CHEMBL279074 Ki = 17.0 nM 7.77
CHEMBL2079656 Ki = 25.0 nM 7.60
CHEMBL370805 COCAINE Ki = 32.0 nM 7.50
CHEMBL2112763 Ki = 85.0 nM 7.07
CHEMBL276332 Ki = 123.0 nM 6.91
CHEMBL19715 Ki = 136.0 nM 6.87
CHEMBL2112762 Ki = 3490.0 nM 5.46