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Assay Detail

CHEMBL1769563

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Functional
Agonist activity at rat mu opioid receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
12
Total Activities
6
Compounds Tested
1
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

Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
Yamamoto T, Nair P, Largent-Milnes TM, Jacobsen NE, Davis P, Ma SW, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
J Med Chem (2011) 54 : 2029 -2038
PubMed 21366266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.41 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766204 2 9.24
CHEMBL1766207 2 9.14
CHEMBL1766206 2 9.08
CHEMBL1766205 2 8.10
CHEMBL1766208 2 7.54
CHEMBL38874 DAMGO 2 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766204 EC50 = 0.5754 nM 9.24
CHEMBL1766204 EC50 = 0.57 nM 9.24
CHEMBL1766207 EC50 = 0.72 nM 9.14
CHEMBL1766206 EC50 = 0.8318 nM 9.08
CHEMBL1766206 EC50 = 0.83 nM 9.08
CHEMBL1766207 EC50 = 0.955 nM 9.02
CHEMBL1766205 EC50 = 7.943 nM 8.10
CHEMBL1766205 EC50 = 8.0 nM 8.10
CHEMBL1766208 EC50 = 28.84 nM 7.54
CHEMBL1766208 EC50 = 29.0 nM 7.54
CHEMBL38874 DAMGO EC50 = 36.31 nM 7.44
CHEMBL38874 DAMGO EC50 = 37.0 nM 7.43