Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL905186

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

Functional
Agonist activity at rat mu opioid receptor expressed in HN9.10 cells assessed by [35S]GTP-gamma-S binding assay
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Yamamoto T, Nair P, Davis P, Ma SW, Navratilova E, Moye S, Tumati S, Lai J, Vanderah TW, Yamamura HI, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 2779 -2786
PubMed 17516639 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 7.26 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439019 2 7.56
CHEMBL389652 2 7.50
CHEMBL389651 2 7.48
CHEMBL229280 2 7.47
CHEMBL38874 DAMGO 2 7.44
CHEMBL426363 2 7.38
CHEMBL2371977 2 7.23
CHEMBL387670 2 6.82
CHEMBL2371978 2 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439019 EC50 = 27.54 nM 7.56
CHEMBL439019 EC50 = 28.0 nM 7.55
CHEMBL389652 EC50 = 31.62 nM 7.50
CHEMBL389652 EC50 = 32.0 nM 7.50
CHEMBL389651 EC50 = 33.0 nM 7.48
CHEMBL389651 EC50 = 33.11 nM 7.48
CHEMBL229280 EC50 = 33.88 nM 7.47
CHEMBL229280 EC50 = 34.0 nM 7.47
CHEMBL38874 DAMGO EC50 = 36.31 nM 7.44
CHEMBL38874 DAMGO EC50 = 37.0 nM 7.43
CHEMBL426363 EC50 = 42.0 nM 7.38
CHEMBL426363 EC50 = 41.69 nM 7.38
CHEMBL2371977 EC50 = 59.0 nM 7.23
CHEMBL2371977 EC50 = 58.88 nM 7.23
CHEMBL387670 EC50 = 150.0 nM 6.82
CHEMBL387670 EC50 = 151.36 nM 6.82
CHEMBL2371978 EC50 = 346.74 nM 6.46
CHEMBL2371978 EC50 = 350.0 nM 6.46