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Assay Detail

CHEMBL2065329

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

Binding
Displacement of [3H]DTG from sigma2 receptor in Sprague-Dawley rat liver membrane after 90 mins by liquid scintillation counting in presence of pentazocine
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7 6.93 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282433 DITOLYLGUANIDINE 1 7.50
CHEMBL54 HALOPERIDOL 4.0 1 7.29
CHEMBL2064617 1 7.17
CHEMBL20943 1 7.06
CHEMBL2064615 1 6.92
CHEMBL2064616 1 6.86
CHEMBL60542 (+)-PENTAZOCINE 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282433 DITOLYLGUANIDINE Ki = 31.7 nM 7.50
CHEMBL54 HALOPERIDOL Ki = 51.6 nM 7.29
CHEMBL2064617 Ki = 68.3 nM 7.17
CHEMBL20943 Ki = 86.7 nM 7.06
CHEMBL2064615 Ki = 118.8 nM 6.92
CHEMBL2064616 Ki = 137.5 nM 6.86
CHEMBL60542 (+)-PENTAZOCINE Ki = 1880.8 nM 5.73