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Assay Detail

CHEMBL5144875

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Toxicity
Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 2 hrs by scintillation counting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Cell Type CHO
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Morphinan derivatives with an oxabicyclo[3.2.1]octane structure as dual agonists toward δ and κ opioid receptors.
Uenohara Y, Tsumura S, Hirayama S, Higashi E, Watanabe Y, Gouda H, Nagase H, Fujii H.
Bioorg Med Chem (2022) 53 : 116552 -116552
PubMed 34894610 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.22 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186730 1 8.56
CHEMBL38874 DAMGO 1 8.45
CHEMBL5200050 1 8.33
CHEMBL5175717 1 8.27
CHEMBL5200992 1 8.25
CHEMBL5185996 1 8.15
CHEMBL5178511 1 8.03
CHEMBL5170301 1 8.03
CHEMBL5200218 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186730 EC50 = 2.72 nM 8.56
CHEMBL38874 DAMGO EC50 = 3.59 nM 8.45
CHEMBL5200050 EC50 = 4.7 nM 8.33
CHEMBL5175717 EC50 = 5.37 nM 8.27
CHEMBL5200992 EC50 = 5.61 nM 8.25
CHEMBL5185996 EC50 = 7.11 nM 8.15
CHEMBL5178511 EC50 = 9.43 nM 8.03
CHEMBL5170301 EC50 = 9.35 nM 8.03
CHEMBL5200218 EC50 = 12.7 nM 7.90