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Assay Detail

CHEMBL5031741

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 membranes after 150 mins by microbeta scintillation counting method
7
Total Activities
7
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 Valproate Ester (<i>S</i>)-(-)-MRJF22: Preliminary Studies as a Potential Multifunctional Agent Against Uveal Melanoma.
Barbaraci C, Giurdanella G, Leotta CG, Longo A, Amata E, Dichiara M, Pasquinucci L, Turnaturi R, Prezzavento O, Cacciatore I, Zuccarello E, Lupo G, Pitari GM, Anfuso CD, Marrazzo A.
J Med Chem (2021) 64 : 13622 -13632
PubMed 34477381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.19 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129159 1 8.70
CHEMBL54 HALOPERIDOL 4.0 1 8.66
CHEMBL1036 HYDROXYHALOPERIDOL 1 8.54
CHEMBL129237 1 8.52
CHEMBL4747257 1 7.89
CHEMBL5079556 1 7.80
CHEMBL5094340 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129159 Ki = 2.0 nM 8.70
CHEMBL54 HALOPERIDOL Ki = 2.2 nM 8.66
CHEMBL1036 HYDROXYHALOPERIDOL Ki = 2.9 nM 8.54
CHEMBL129237 Ki = 3.0 nM 8.52
CHEMBL4747257 Ki = 13.0 nM 7.89
CHEMBL5079556 Ki = 16.0 nM 7.80
CHEMBL5094340 Ki = 64.0 nM 7.19