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Assay Detail

CHEMBL3590744

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Binding
Displacement of (-)-[3H]vesamicol from VAChT in Sprague-Dawley rat brain membranes incubated for 2 hrs by liquid scintillation counting based competitive radioligand binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vesicular acetylcholine transporter (CHEMBL2125)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
Barthel C, Sorger D, Deuther-Conrad W, Scheunemann M, Schweiger S, Jäckel P, Roghani A, Steinbach J, Schüürmann G, Sabri O, Brust P, Wenzel B.
Eur J Med Chem (2015) 100 : 50 -67
PubMed 26071858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.36 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87379 BENZOVESAMICOL 1 7.63
CHEMBL20730 VESAMICOL 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87379 BENZOVESAMICOL Ki = 23.4 nM 7.63
CHEMBL20730 VESAMICOL Ki = 84.2 nM 7.08