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Assay Detail

CHEMBL2424424

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

Binding
Antagonist activity at mu/kappa opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Ileum
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

mu/kappa opioid receptor (CHEMBL3038518)
Type PROTEIN FAMILY
Organism Cavia porcellus

Publication

N-terminal guanidinylation of TIPP (Tyr-Tic-Phe-Phe) peptides results in major changes of the opioid activity profile.
Weltrowska G, Nguyen TM, Chung NN, Wilkes BC, Schiller PW.
Bioorg Med Chem Lett (2013) 23 : 5082 -5085
PubMed 23932788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.98 5.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3038186 1 5.98
CHEMBL571492 1 -
CHEMBL538700 1 -
CHEMBL3038184 1 -
CHEMBL3038183 1 -
CHEMBL3038182 1 -
CHEMBL555206 1 -
CHEMBL191751 1 -
CHEMBL3038187 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3038186 IC50 = 1050.0 nM 5.98
CHEMBL571492 IC50 - -
CHEMBL538700 IC50 - -
CHEMBL3038184 IC50 - -
CHEMBL3038183 IC50 - -
CHEMBL3038182 IC50 - -
CHEMBL555206 IC50 - -
CHEMBL191751 IC50 - -
CHEMBL3038187 IC50 - -