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Assay Detail

CHEMBL1111778

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

Binding
Displacement of [3H]DTG from sigma 2 receptor in rat liver membrane homogenates after 2 hrs by liquid scintillation counting
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter.
Efange SM, Khare AB, von Hohenberg K, Mach RH, Parsons SM, Tu Z.
J Med Chem (2010) 53 : 2825 -2835
PubMed 20218624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.01 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204032 1 7.52
CHEMBL20730 VESAMICOL 1 7.46
CHEMBL1204034 1 7.45
CHEMBL1204035 1 7.31
CHEMBL1204037 1 7.14
CHEMBL1204031 1 6.95
CHEMBL1204045 1 6.92
CHEMBL1204030 1 6.47
CHEMBL1204038 1 6.46
CHEMBL1204043 1 6.45
CHEMBL1204039 1 -
CHEMBL1204040 1 -
CHEMBL1204041 1 -
CHEMBL1204042 1 -
CHEMBL1204044 1 -
CHEMBL1204046 1 -
CHEMBL1204047 1 -
CHEMBL1204048 1 -
CHEMBL1204049 1 -
CHEMBL1204050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204032 Ki = 30.13 nM 7.52
CHEMBL20730 VESAMICOL Ki = 34.5 nM 7.46
CHEMBL1204034 Ki = 35.73 nM 7.45
CHEMBL1204035 Ki = 48.86 nM 7.31
CHEMBL1204037 Ki = 72.02 nM 7.14
CHEMBL1204031 Ki = 112.74 nM 6.95
CHEMBL1204045 Ki = 120.66 nM 6.92
CHEMBL1204030 Ki = 341.4 nM 6.47
CHEMBL1204038 Ki = 344.5 nM 6.46
CHEMBL1204043 Ki = 352.7 nM 6.45
CHEMBL1204039 Ki > 1000.0 nM -
CHEMBL1204040 Ki > 1000.0 nM -
CHEMBL1204041 Ki > 1000.0 nM -
CHEMBL1204042 Ki > 1000.0 nM -
CHEMBL1204044 Ki > 1000.0 nM -
CHEMBL1204046 Ki > 1000.0 nM -
CHEMBL1204047 Ki > 1000.0 nM -
CHEMBL1204048 Ki > 1000.0 nM -
CHEMBL1204049 Ki > 1000.0 nM -
CHEMBL1204050 Ki > 1000.0 nM -