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Assay Detail

CHEMBL4705239

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Functional
Agonist activity at MOR/DOR in wild-type C57BL6 mouse spinal cord membranes assessed as stimulation of [35S]-GTPgammaS binding measured after 60 mins by scintillation counting assay
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Spinal cord
Subcellular Cell membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Opioid receptors; mu and delta (CHEMBL2221343)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Synthesis and Pharmacology of a Novel μ-δ Opioid Receptor Heteromer-Selective Agonist Based on the Carfentanyl Template.
Faouzi A,Uprety R,Gomes I,Massaly N,Keresztes AI,Le Rouzic V,Gupta A,Zhang T,Yoon HJ,Ansonoff M,Allaoa A,Pan YX,Pintar J,Morón JA,Streicher JM,Devi LA,Majumdar S
J Med Chem (2020) 63 : 13618 -13637
PubMed 33170687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 9.27 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4795492 2 10.50
CHEMBL20226 DELTORPHIN II 2 8.75
CHEMBL38874 DAMGO 2 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4795492 EC50 = 0.03162 nM 10.50
CHEMBL4795492 EC50 = 0.0348 nM 10.46
CHEMBL20226 DELTORPHIN II EC50 = 1.78 nM 8.75
CHEMBL20226 DELTORPHIN II EC50 = 1.778 nM 8.75
CHEMBL38874 DAMGO EC50 = 2.69 nM 8.57
CHEMBL38874 DAMGO EC50 = 2.692 nM 8.57