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Assay Detail

CHEMBL893247

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Functional
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding after 60 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
Bioorg Med Chem (2007) 15 : 4106 -4112
PubMed 17433695 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.10 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 9.72
CHEMBL301160 BUTORPHAN 1 8.89
CHEMBL428038 1 8.08
CHEMBL242968 1 7.48
CHEMBL290543 1 7.34
CHEMBL394573 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN EC50 = 0.19 nM 9.72
CHEMBL301160 BUTORPHAN EC50 = 1.3 nM 8.89
CHEMBL428038 EC50 = 8.4 nM 8.08
CHEMBL242968 EC50 = 33.0 nM 7.48
CHEMBL290543 EC50 = 46.0 nM 7.34
CHEMBL394573 EC50 = 87.0 nM 7.06