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Assay Detail

CHEMBL677366

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

Binding
Binding affinity at dopamine transporter in rat brain by [3H]WIN-35428 displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
Kulkarni SS, Grundt P, Kopajtic T, Katz JL, Newman AH.
J Med Chem (2004) 47 : 3388 -3398
PubMed 15189035 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.46 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112280 1 9.05
CHEMBL543876 1 8.43
CHEMBL2308105 1 8.07
CHEMBL317757 DIFLUOROBENZTROPINE 1 7.93
CHEMBL112528 1 7.90
CHEMBL115253 1 7.88
CHEMBL3085021 1 7.86
CHEMBL3084884 1 7.70
CHEMBL115311 1 7.58
CHEMBL3085020 1 7.56
CHEMBL324518 1 7.44
CHEMBL326706 1 7.37
CHEMBL115370 1 7.32
CHEMBL325826 1 7.31
CHEMBL327055 1 7.18
CHEMBL326604 1 6.74
CHEMBL370805 COCAINE 4.0 1 6.54
CHEMBL111928 1 6.15
CHEMBL115710 1 5.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112280 Ki = 0.9 nM 9.05
CHEMBL543876 Ki = 3.7 nM 8.43
CHEMBL2308105 Ki = 8.51 nM 8.07
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 11.8 nM 7.93
CHEMBL112528 Ki = 12.6 nM 7.90
CHEMBL115253 Ki = 13.1 nM 7.88
CHEMBL3085021 Ki = 13.9 nM 7.86
CHEMBL3084884 Ki = 20.0 nM 7.70
CHEMBL115311 Ki = 26.0 nM 7.58
CHEMBL3085020 Ki = 27.6 nM 7.56
CHEMBL324518 Ki = 36.0 nM 7.44
CHEMBL326706 Ki = 42.6 nM 7.37
CHEMBL115370 Ki = 48.0 nM 7.32
CHEMBL325826 Ki = 48.5 nM 7.31
CHEMBL327055 Ki = 65.9 nM 7.18
CHEMBL326604 Ki = 181.0 nM 6.74
CHEMBL370805 COCAINE Ki = 285.0 nM 6.54
CHEMBL111928 Ki = 703.0 nM 6.15
CHEMBL115710 Ki = 1620.0 nM 5.79