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Assay Detail

CHEMBL4000617

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

Binding
Displacement of [3H]-PTZ from sigma1 receptor in guinea pig brain membranes after 150 mins in presence of 250 uM DPH by liquid scintillation counting method
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

(+)-and (-)-Phenazocine enantiomers: Evaluation of their dual opioid agonist/σ1 antagonist properties and antinociceptive effects.
Prezzavento O, Arena E, Sánchez-Fernández C, Turnaturi R, Parenti C, Marrazzo A, Catalano R, Amata E, Pasquinucci L, Cobos EJ.
Eur J Med Chem (2017) 125 : 603 -610
PubMed 27721146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.88 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.57
CHEMBL1449159 1 7.18
CHEMBL316632 1 -
CHEMBL94350 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.7 nM 8.57
CHEMBL1449159 Ki = 66.6 nM 7.18
CHEMBL316632 Ki - -
CHEMBL94350 Ki - -