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Assay Detail

CHEMBL687456

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

Functional
Compound was evaluated for kappa opioid receptor mediated agonistic effect in electrically stimulated guinea-pig ileum
4
Total Activities
4
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 Intermediate

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

6N-Cinnamoyl--naltrexamine and its p-nitro derivative. High efficacy -opioid agonists with weak antagonist actions
Derrick I, Moynihan HA, Broadbear J, Woods JH, Lewis JW
Bioorg Med Chem Lett (1996) 6 : 167 -172
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.46 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473362 1 9.40
CHEMBL296693 1 8.66
CHEMBL297756 1 7.90
CHEMBL417535 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473362 IC50 = 0.4 nM 9.40
CHEMBL296693 IC50 = 2.2 nM 8.66
CHEMBL297756 IC50 = 12.6 nM 7.90
CHEMBL417535 IC50 = 13.4 nM 7.87