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Assay Detail

CHEMBL871087

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

Functional
Antagonist activity at mu opioid receptor assessed as inhibition of endomorphin-2-induced contraction of guinea pig ileum
3
Total Activities
3
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

Effect of lysine at C-terminus of the Dmt-Tic opioid pharmacophore.
Balboni G, Onnis V, Congiu C, Zotti M, Sasaki Y, Ambo A, Bryant SD, Jinsmaa Y, Lazarus LH, Trapella C, Salvadori S.
J Med Chem (2006) 49 : 5610 -5617
PubMed 16942034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 7.31 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028968 1 8.16
CHEMBL2028969 1 7.96
CHEMBL2028967 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028968 Kd = 6.918 nM 8.16
CHEMBL2028969 Kd = 10.96 nM 7.96
CHEMBL2028967 Kd = 1513.56 nM 5.82