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Assay Detail

CHEMBL2065327

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

Binding
Displacement of (-)-[3H]vesamicol from VAChT in Sprague-Dawley rat cerebral membrane after 60 mins by liquid scintillation counting in presence of DTG
4
Total Activities
4
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

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

Publication

Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT).
Kozaka T, Uno I, Kitamura Y, Miwa D, Ogawa K, Shiba K.
Bioorg Med Chem (2012) 20 : 4936 -4941
PubMed 22831799 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.72 7.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064617 1 7.87
CHEMBL2064616 1 7.86
CHEMBL2064615 1 7.69
CHEMBL20943 1 7.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064617 Ki = 13.6 nM 7.87
CHEMBL2064616 Ki = 13.8 nM 7.86
CHEMBL2064615 Ki = 20.5 nM 7.69
CHEMBL20943 Ki = 33.9 nM 7.47