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Assay Detail

CHEMBL5377589

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 membrane by radioligand binding assay
2
Total Activities
2
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

A Novel Bifunctional μOR Agonist and σ<sub>1</sub>R Antagonist with Potent Analgesic Responses and Reduced Adverse Effects.
Miao Z, Zhong Y, Gan Y, Fu K, Liu W, Cao Z, Zhao T, Li Z, Hai A, Peng Y, Zuo Z, Zhang T, Hu S, Chen C, Kang T, Huang T, Guo D, Ke B.
J Med Chem (2023) 66 : 16257 -16275
PubMed 38015878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.76 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5415173 1 6.44
CHEMBL5418375 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5415173 Ki = 363.7 nM 6.44
CHEMBL5418375 Ki = 8300.0 nM 5.08