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Assay Detail

CHEMBL919396

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Functional
Agonist activity at human opioid gamma receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
J Med Chem (2007) 50 : 2254 -2258
PubMed 17407276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.20 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301160 BUTORPHAN 1 8.80
CHEMBL2113275 1 8.70
CHEMBL383320 1 8.52
CHEMBL224014 1 8.36
CHEMBL895 NALBUPHINE 4.0 1 7.85
CHEMBL38874 DAMGO 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301160 BUTORPHAN EC50 = 1.6 nM 8.80
CHEMBL2113275 EC50 = 2.0 nM 8.70
CHEMBL383320 EC50 = 3.0 nM 8.52
CHEMBL224014 EC50 = 4.4 nM 8.36
CHEMBL895 NALBUPHINE EC50 = 14.0 nM 7.85
CHEMBL38874 DAMGO EC50 = 110.0 nM 6.96