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Assay Detail

CHEMBL1024704

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

Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells by [35S]GTPgammaS binding assay
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Yamamoto T, Nair P, Jacobsen NE, Davis P, Ma SW, Navratilova E, Moye S, Lai J, Yamamura HI, Vanderah TW, Porreca F, Hruby VJ.
J Med Chem (2008) 51 : 6334 -6347
PubMed 18821747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.69 8.15
pEC50 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL507340 2 8.15
CHEMBL448998 2 7.68
CHEMBL389652 2 7.50
CHEMBL38874 DAMGO 2 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL507340 EC50 = 7.0 nM 8.15
CHEMBL448998 EC50 = 21.0 nM 7.68
CHEMBL389652 EC50 = 32.0 nM 7.50
CHEMBL38874 DAMGO EC50 = 37.0 nM 7.43
CHEMBL389652 pEC50 = 7.5 nM -
CHEMBL38874 DAMGO pEC50 = 7.4 nM -
CHEMBL448998 pEC50 = 7.7 nM -
CHEMBL507340 pEC50 = 8.2 nM -