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Assay Detail

CHEMBL4705243

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Binding
Agonist activity at EA-fragment beta-arrestin-tagged human DOR expressed in human U2OS cell membranes assessed as stimulation beta-arrestin recruitment after 60 mins by Pathhunter chemiluminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U2OS
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

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 11 6.48 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20226 DELTORPHIN II 1 8.10
CHEMBL4781906 1 6.29
CHEMBL1612697 1 6.09
CHEMBL4795492 1 6.02
CHEMBL4788377 1 5.89
CHEMBL38874 DAMGO 1 -
CHEMBL4760974 1 -
CHEMBL4758061 1 -
CHEMBL4761310 1 -
CHEMBL4776176 1 -
CHEMBL4783765 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20226 DELTORPHIN II EC50 = 8.0 nM 8.10
CHEMBL4781906 EC50 = 509.0 nM 6.29
CHEMBL1612697 EC50 = 812.0 nM 6.09
CHEMBL4795492 EC50 = 960.0 nM 6.02
CHEMBL4788377 EC50 = 1296.0 nM 5.89
CHEMBL38874 DAMGO EC50 - -
CHEMBL4760974 EC50 - -
CHEMBL4758061 EC50 - -
CHEMBL4761310 EC50 - -
CHEMBL4776176 EC50 - -
CHEMBL4783765 EC50 - -