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Assay Detail

CHEMBL864803

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Functional
Agonist activity at mu opioid receptor by guinea pig ileum assay
7
Total Activities
7
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 Expert

Target

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

Publication

New 2',6'-dimethyl-L-tyrosine (Dmt) opioid peptidomimetics based on the Aba-Gly scaffold. Development of unique mu-opioid receptor ligands.
Ballet S, Salvadori S, Trapella C, Bryant SD, Jinsmaa Y, Lazarus LH, Negri L, Giannini E, Lattanzi R, Tourwé D, Balboni G.
J Med Chem (2006) 49 : 3990 -3993
PubMed 16789756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.65 8.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL501451 1 8.59
CHEMBL458631 1 8.57
CHEMBL333357 ENDOMORPHIN 2 1 7.86
CHEMBL2375157 1 7.57
CHEMBL208683 1 7.29
CHEMBL377392 1 7.02
CHEMBL211543 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL501451 IC50 = 2.57 nM 8.59
CHEMBL458631 IC50 = 2.69 nM 8.57
CHEMBL333357 ENDOMORPHIN 2 IC50 = 13.7 nM 7.86
CHEMBL2375157 IC50 = 26.9 nM 7.57
CHEMBL208683 IC50 = 51.0 nM 7.29
CHEMBL377392 IC50 = 95.0 nM 7.02
CHEMBL211543 IC50 = 231.0 nM 6.64