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Assay Detail

CHEMBL839628

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

Binding
Inhibition of [3H]-nisoxetine binding to Norepinephrine transporter from rat cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Andrés JI, Alcázar J, Alonso JM, Alvarez RM, Bakker MH, Biesmans I, Cid JM, De Lucas AI, Fernández J, Font LM, Hens KA, Iturrino L, Lenaerts I, Martínez S, Megens AA, Pastor J, Vermote PC, Steckler T.
J Med Chem (2005) 48 : 2054 -2071
PubMed 15771448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.77 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92860 1 7.48
CHEMBL91157 1 6.75
CHEMBL419316 1 6.66
CHEMBL328114 1 6.51
CHEMBL90997 1 6.44
CHEMBL268258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92860 Ki = 33.0 nM 7.48
CHEMBL91157 Ki = 177.0 nM 6.75
CHEMBL419316 Ki = 220.0 nM 6.66
CHEMBL328114 Ki = 312.0 nM 6.51
CHEMBL90997 Ki = 365.0 nM 6.44
CHEMBL268258 Ki > 1000.0 nM -