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Assay Detail

CHEMBL4252134

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Functional
Antagonist activity at kappa opioid receptor (unknown origin) assessed as stimulation of [35S]GTPgammaS
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Kappa-type opioid receptor (CHEMBL237)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective kappa opioid antagonists for treatment of addiction, are we there yet?
Helal MA, Habib ES, Chittiboyina AG.
Eur J Med Chem (2017) 141 : 632 -647
PubMed 29107424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 10.70 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415247 JDTIC 1.0 1 11.00
CHEMBL511142 BUPRENORPHINE 4.0 1 10.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415247 JDTIC Ki = 0.01 nM 11.00
CHEMBL511142 BUPRENORPHINE Ki = 0.04 nM 10.40