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Assay Detail

CHEMBL1274064

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

Binding
Displacement of (-)-[3H]pentazocine from sigma 1 receptor in rat cortical membranes after 120 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

3D QSAR study, synthesis, and in vitro evaluation of (+)-5-FBVM as potential PET radioligand for the vesicular acetylcholine transporter (VAChT).
Kovac M, Mavel S, Deuther-Conrad W, Méheux N, Glöckner J, Wenzel B, Anderluh M, Brust P, Guilloteau D, Emond P.
Bioorg Med Chem (2010) 18 : 7659 -7667
PubMed 20889347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.11 8.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1271961 1 8.45
CHEMBL1271906 1 7.88
CHEMBL1271907 1 7.42
CHEMBL1271793 1 6.68
CHEMBL65239 1 6.58
CHEMBL1271850 1 6.57
CHEMBL277630 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1271961 Ki = 3.57 nM 8.45
CHEMBL1271906 Ki = 13.2 nM 7.88
CHEMBL1271907 Ki = 38.1 nM 7.42
CHEMBL1271793 Ki = 209.0 nM 6.68
CHEMBL65239 Ki = 266.0 nM 6.58
CHEMBL1271850 Ki = 269.0 nM 6.57
CHEMBL277630 Ki = 652.0 nM 6.19