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Assay Detail

CHEMBL1056149

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Functional
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
7
Total Activities
7
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 Intermediate

Target

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

Publication

Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands.
Decker M, Fulton BS, Zhang B, Knapp BI, Bidlack JM, Neumeyer JL.
J Med Chem (2009) 52 : 7389 -7396
PubMed 19634902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.56 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147511 1 9.07
CHEMBL301160 BUTORPHAN 1 8.89
CHEMBL584791 1 8.80
CHEMBL566346 1 8.55
CHEMBL565679 1 8.31
CHEMBL584790 1 8.19
CHEMBL582930 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147511 EC50 = 0.85 nM 9.07
CHEMBL301160 BUTORPHAN EC50 = 1.3 nM 8.89
CHEMBL584791 EC50 = 1.6 nM 8.80
CHEMBL566346 EC50 = 2.8 nM 8.55
CHEMBL565679 EC50 = 4.9 nM 8.31
CHEMBL584790 EC50 = 6.4 nM 8.19
CHEMBL582930 EC50 = 7.3 nM 8.14