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Assay Detail

CHEMBL823202

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

Binding
Compound was evaluated for binding affinity against [3H]- bremazocine labeled kappa2 opioid receptor in guinea-pig brain homogenate.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

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
Ki 5 7.34 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473362 1 7.89
CHEMBL417535 1 7.52
CHEMBL296693 1 7.32
CHEMBL473136 1 7.18
CHEMBL297756 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473362 Ki = 12.8 nM 7.89
CHEMBL417535 Ki = 30.5 nM 7.52
CHEMBL296693 Ki = 48.3 nM 7.32
CHEMBL473136 Ki = 66.5 nM 7.18
CHEMBL297756 Ki = 171.4 nM 6.77