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Assay Detail

CHEMBL890739

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

Binding
Displacement of [3H]nisoxetine from NET in Sprague-Dawley rat brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Gong PK, Blough BE, Brieaddy LE, Huang X, Kuhar MJ, Navarro HA, Carroll FI.
J Med Chem (2007) 50 : 3686 -3695
PubMed 17602602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.56 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL390742 TROPARIL 1 6.04
CHEMBL227179 1 5.07
CHEMBL390743 1 -
CHEMBL2113279 1 -
CHEMBL376113 1 -
CHEMBL226933 1 -
CHEMBL226984 1 -
CHEMBL229436 1 -
CHEMBL436132 1 -
CHEMBL229381 1 -
CHEMBL229699 1 -
CHEMBL388832 1 -
CHEMBL388612 1 -
CHEMBL227233 1 -
CHEMBL388760 1 -
CHEMBL227232 1 -
CHEMBL227231 1 -
CHEMBL388759 1 -
CHEMBL227180 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL390742 TROPARIL Ki = 920.0 nM 6.04
CHEMBL227179 Ki = 8560.0 nM 5.07
CHEMBL390743 Ki > 2000.0 nM -
CHEMBL2113279 Ki > 2000.0 nM -
CHEMBL376113 Ki > 2000.0 nM -
CHEMBL226933 Ki > 2000.0 nM -
CHEMBL226984 Ki > 2000.0 nM -
CHEMBL229436 Ki > 2000.0 nM -
CHEMBL436132 Ki > 2000.0 nM -
CHEMBL229381 Ki > 2000.0 nM -
CHEMBL229699 Ki > 2000.0 nM -
CHEMBL388832 Ki > 2000.0 nM -
CHEMBL388612 Ki > 2000.0 nM -
CHEMBL227233 Ki > 2000.0 nM -
CHEMBL388760 Ki > 2000.0 nM -
CHEMBL227232 Ki > 2000.0 nM -
CHEMBL227231 Ki > 2000.0 nM -
CHEMBL388759 Ki > 2000.0 nM -
CHEMBL227180 Ki > 2000.0 nM -