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Assay Detail

CHEMBL869901

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

Functional
Agonist activity at mu opioid receptor assessed as inhibition of electrically-evoked contraction of guinea pig ileum
11
Total Activities
11
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
IC50 11 6.79 7.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333357 ENDOMORPHIN 2 1 7.86
CHEMBL3143821 1 7.40
CHEMBL3143820 1 7.27
CHEMBL3143819 1 7.20
CHEMBL3143818 1 6.43
CHEMBL2028970 1 6.36
CHEMBL2028972 1 5.90
CHEMBL2028971 1 5.90
CHEMBL2028967 1 -
CHEMBL2028969 1 -
CHEMBL2028968 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333357 ENDOMORPHIN 2 IC50 = 13.7 nM 7.86
CHEMBL3143821 IC50 = 39.7 nM 7.40
CHEMBL3143820 IC50 = 53.9 nM 7.27
CHEMBL3143819 IC50 = 62.5 nM 7.20
CHEMBL3143818 IC50 = 375.0 nM 6.43
CHEMBL2028970 IC50 = 438.0 nM 6.36
CHEMBL2028972 IC50 = 1254.0 nM 5.90
CHEMBL2028971 IC50 = 1248.0 nM 5.90
CHEMBL2028967 IC50 > 10000.0 nM -
CHEMBL2028969 IC50 > 10000.0 nM -
CHEMBL2028968 IC50 > 10000.0 nM -