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Assay Detail

CHEMBL4681286

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

Binding
Displacement of [3H]-pentazocine from sigma1 receptor in guinea pig brain membranes by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Cell 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

Antiangiogenic Effect of (±)-Haloperidol Metabolite II Valproate Ester [(±)-MRJF22] in Human Microvascular Retinal Endothelial Cells.
Olivieri M,Amata E,Vinciguerra S,Fiorito J,Giurdanella G,Drago F,Caporarello N,Prezzavento O,Arena E,Salerno L,Rescifina A,Lupo G,Anfuso CD,Marrazzo A
J Med Chem (2016) 59 : 9960 -9966
PubMed 27739690 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.33 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.57
CHEMBL1036 HYDROXYHALOPERIDOL 1 8.54
CHEMBL4747257 1 7.89
CHEMBL109 VALPROIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.7 nM 8.57
CHEMBL1036 HYDROXYHALOPERIDOL Ki = 2.9 nM 8.54
CHEMBL4747257 Ki = 13.0 nM 7.89
CHEMBL109 VALPROIC ACID Ki > 10000.0 nM -