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Assay Detail

CHEMBL817829

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

Binding
Displacement of [3H]vesamicol from Vesicular Acetylcholine Transporter (VAChT)
14
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Vesicular acetylcholine transporter (CHEMBL4767)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
Efange SM, Khare AB, Mach RH, Parsons SM.
J Med Chem (1999) 42 : 2862 -2869
PubMed 10425095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.43 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50880 1 9.89
CHEMBL330635 2 9.59
CHEMBL97524 2 9.52
CHEMBL95701 1 9.40
CHEMBL316520 3 9.36
CHEMBL95857 1 9.00
CHEMBL20730 VESAMICOL 1 8.70
CHEMBL330386 1 8.28
CHEMBL318675 1 8.00
CHEMBL94733 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50880 Ki = 0.13 nM 9.89
CHEMBL330635 Ki = 0.26 nM 9.59
CHEMBL97524 Ki = 0.3 nM 9.52
CHEMBL95701 Ki = 0.4 nM 9.40
CHEMBL316520 Ki = 0.44 nM 9.36
CHEMBL95857 Ki = 0.99 nM 9.00
CHEMBL20730 VESAMICOL Ki = 2.0 nM 8.70
CHEMBL330386 Ki = 5.2 nM 8.28
CHEMBL330635 Ki = 7.7 nM 8.11
CHEMBL318675 Ki = 10.0 nM 8.00
CHEMBL97524 Ki = 13.1 nM 7.88
CHEMBL316520 Ki = 21.0 nM 7.68
CHEMBL316520 Ki = 96.0 nM 7.02
CHEMBL94733 Ki = 2900.0 nM 5.54