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Assay Detail

CHEMBL1769559

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Functional
Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

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
IC50 6 7.54 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.06
CHEMBL1766208 1 7.72
CHEMBL1766206 1 7.66
CHEMBL1766207 1 7.64
CHEMBL1766204 1 7.17
CHEMBL1766205 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN IC50 = 8.8 nM 8.06
CHEMBL1766208 IC50 = 19.0 nM 7.72
CHEMBL1766206 IC50 = 22.0 nM 7.66
CHEMBL1766207 IC50 = 23.0 nM 7.64
CHEMBL1766204 IC50 = 68.0 nM 7.17
CHEMBL1766205 IC50 = 110.0 nM 6.96