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Assay Detail

CHEMBL755494

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

Binding
Effect on binding to wild-type opioid receptor kappa 1 using [3H]diprenorphine in transiently expressed rat HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL3614)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
Sharma SK, Jones RM, Metzger TG, Ferguson DM, Portoghese PS.
J Med Chem (2001) 44 : 2073 -2079
PubMed 11405645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.71 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE 1 9.68
CHEMBL610279 1 8.95
CHEMBL610280 1 7.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485832 GUANIDINONALTRINDOLE Ki = 0.21 nM 9.68
CHEMBL610279 Ki = 1.13 nM 8.95
CHEMBL610280 Ki = 32.7 nM 7.49