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Assay Detail

CHEMBL3590746

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

Binding
Displacement of (-)-[3H]vesamicol from VAChT in Torpedo californica electric organ synaptic vesicles
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo californica
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vesicular acetylcholine transporter (CHEMBL3313)
Type SINGLE PROTEIN
Organism Torpedo californica

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 5 9.11 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87381 1 10.89
CHEMBL87379 BENZOVESAMICOL 1 10.26
CHEMBL264437 1 9.47
CHEMBL473129 1 8.57
CHEMBL1089853 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87381 Ki = 0.013 nM 10.89
CHEMBL87379 BENZOVESAMICOL Ki = 0.055 nM 10.26
CHEMBL264437 Ki = 0.34 nM 9.47
CHEMBL473129 Ki = 2.7 nM 8.57
CHEMBL1089853 Ki = 423.0 nM 6.37