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Assay Detail

CHEMBL800350

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

Functional
Compound was tested for inhibition of [3H]dopamine uptake (DAUI) in rat synaptosomes
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
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
IC50 14 7.50 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085020 1 8.30
CHEMBL115253 1 8.19
CHEMBL324518 1 8.09
CHEMBL317757 DIFLUOROBENZTROPINE 1 7.86
CHEMBL112528 1 7.85
CHEMBL327055 1 7.73
CHEMBL325826 1 7.65
CHEMBL3084884 1 7.63
CHEMBL3085021 1 7.58
CHEMBL2308105 1 7.41
CHEMBL326706 1 7.31
CHEMBL111928 1 6.64
CHEMBL370805 COCAINE 4.0 1 6.63
CHEMBL115710 1 6.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085020 IC50 = 5.0 nM 8.30
CHEMBL115253 IC50 = 6.5 nM 8.19
CHEMBL324518 IC50 = 8.1 nM 8.09
CHEMBL317757 DIFLUOROBENZTROPINE IC50 = 13.8 nM 7.86
CHEMBL112528 IC50 = 14.2 nM 7.85
CHEMBL327055 IC50 = 18.7 nM 7.73
CHEMBL325826 IC50 = 22.3 nM 7.65
CHEMBL3084884 IC50 = 23.4 nM 7.63
CHEMBL3085021 IC50 = 26.0 nM 7.58
CHEMBL2308105 IC50 = 39.0 nM 7.41
CHEMBL326706 IC50 = 48.9 nM 7.31
CHEMBL111928 IC50 = 227.0 nM 6.64
CHEMBL370805 COCAINE IC50 = 236.0 nM 6.63
CHEMBL115710 IC50 = 659.0 nM 6.18