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Assay Detail

CHEMBL4186334

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Binding
Inhibition of [3H]dopamine uptake at VMAT2 in rat synaptic vesicles after 8 mins by liquid scintillation spectrometry
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Synaptic vesicular amine transporter (CHEMBL4828)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2.
Hankosky ER, Joolakanti SR, Nickell JR, Janganati V, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2017) 27 : 5467 -5472
PubMed 29153425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.35 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333465 LOBELANE 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333465 LOBELANE Ki = 45.0 nM 7.35