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Assay Detail

CHEMBL3396041

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

Binding
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor guinea pig brain membranes incubated for 150 mins by scintillation counting method
6
Total Activities
6
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

Haloperidol metabolite II prodrug: asymmetric synthesis and biological evaluation on rat C6 glioma cells.
Sozio P, Fiorito J, Di Giacomo V, Di Stefano A, Marinelli L, Cacciatore I, Cataldi A, Pacella S, Turkez H, Parenti C, Rescifina A, Marrazzo A.
Eur J Med Chem (2015) 90 : 1 -9
PubMed 25461306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.78 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129159 1 8.70
CHEMBL54 HALOPERIDOL 4.0 1 8.60
CHEMBL129237 1 8.52
CHEMBL282433 DITOLYLGUANIDINE 1 7.15
CHEMBL3393789 1 7.06
CHEMBL3393790 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129159 Ki = 2.0 nM 8.70
CHEMBL54 HALOPERIDOL Ki = 2.5 nM 8.60
CHEMBL129237 Ki = 3.0 nM 8.52
CHEMBL282433 DITOLYLGUANIDINE Ki = 70.1 nM 7.15
CHEMBL3393789 Ki = 87.5 nM 7.06
CHEMBL3393790 Ki = 230.0 nM 6.64