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Assay Detail

CHEMBL887394

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Functional
Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding
12
Total Activities
12
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

High-affinity carbamate analogues of morphinan at opioid receptors.
Peng X, Knapp BI, Bidlack JM, Neumeyer JL.
Bioorg Med Chem Lett (2007) 17 : 1508 -1511
PubMed 17276685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.44 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 9.72
CHEMBL397035 1 9.42
CHEMBL263096 1 8.96
CHEMBL427862 1 8.92
CHEMBL301160 BUTORPHAN 1 8.89
CHEMBL242048 1 8.66
CHEMBL394624 1 8.33
CHEMBL242046 1 8.02
CHEMBL241824 1 7.80
CHEMBL242047 1 7.64
CHEMBL245049 1 7.54
CHEMBL290543 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN EC50 = 0.19 nM 9.72
CHEMBL397035 EC50 = 0.38 nM 9.42
CHEMBL263096 EC50 = 1.1 nM 8.96
CHEMBL427862 EC50 = 1.2 nM 8.92
CHEMBL301160 BUTORPHAN EC50 = 1.3 nM 8.89
CHEMBL242048 EC50 = 2.2 nM 8.66
CHEMBL394624 EC50 = 4.7 nM 8.33
CHEMBL242046 EC50 = 9.6 nM 8.02
CHEMBL241824 EC50 = 16.0 nM 7.80
CHEMBL242047 EC50 = 23.0 nM 7.64
CHEMBL245049 EC50 = 29.0 nM 7.54
CHEMBL290543 EC50 = 46.0 nM 7.34