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Assay Detail

CHEMBL1663953

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

Binding
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in guinea pig brain membrane after 150 mins by liquid 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 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

Antiproliferative activity of phenylbutyrate ester of haloperidol metabolite II [(±)-MRJF4] in prostate cancer cells.
Marrazzo A, Fiorito J, Zappalà L, Prezzavento O, Ronsisvalle S, Pasquinucci L, Scoto GM, Bernardini R, Ronsisvalle G.
Eur J Med Chem (2011) 46 : 433 -438
PubMed 21055848 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.03 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.66
CHEMBL1036 HYDROXYHALOPERIDOL 1 8.64
CHEMBL1649601 1 6.79
CHEMBL1469 PHENYLBUTANOIC ACID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 2.2 nM 8.66
CHEMBL1036 HYDROXYHALOPERIDOL Ki = 2.3 nM 8.64
CHEMBL1649601 Ki = 162.0 nM 6.79
CHEMBL1469 PHENYLBUTANOIC ACID Ki > 10000.0 nM -