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Assay Detail

CHEMBL746905

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Binding
Binding affinity for Norepinephrine transporter is assessed from the ability to displace [3H]nisoxetine from rat frontal cortex
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Frontal cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Norepinephrine transporter (CHEMBL304)
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 4 6.09 6.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112763 1 6.67
CHEMBL19944 1 6.57
CHEMBL2079577 1 6.33
CHEMBL2112762 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112763 Ki = 214.0 nM 6.67
CHEMBL19944 Ki = 271.0 nM 6.57
CHEMBL2079577 Ki = 464.0 nM 6.33
CHEMBL2112762 Ki = 16800.0 nM 4.78