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Assay Detail

CHEMBL917909

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]DAMGO from human opioid gamma receptor expressed in CHO cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 7 9.38 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301160 BUTORPHAN 1 9.64
CHEMBL19019 NALTREXONE 4.0 1 9.64
CHEMBL224014 1 9.54
CHEMBL2113275 1 9.37
CHEMBL224671 1 9.34
CHEMBL80 NALOXONE 4.0 1 9.10
CHEMBL895 NALBUPHINE 4.0 1 9.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301160 BUTORPHAN Ki = 0.23 nM 9.64
CHEMBL19019 NALTREXONE Ki = 0.23 nM 9.64
CHEMBL224014 Ki = 0.29 nM 9.54
CHEMBL2113275 Ki = 0.43 nM 9.37
CHEMBL224671 Ki = 0.46 nM 9.34
CHEMBL80 NALOXONE Ki = 0.79 nM 9.10
CHEMBL895 NALBUPHINE Ki = 0.89 nM 9.05