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Assay Detail

CHEMBL753316

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

Functional
Inhibition of Forskolin-Stimulated Adenylyl Cyclase in CHO cells expressing Opioid receptor kappa 1
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Effects of the substitution of Phe4 in the opioid peptide [D-Ala8]dynorphin A-(1-11)NH2.
Vig BS, Zheng MQ, Murray TF, Aldrich JV.
J Med Chem (2003) 46 : 4002 -4008
PubMed 12954053 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.51 8.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405057 1 8.91
CHEMBL412228 1 8.45
CHEMBL413832 1 8.28
CHEMBL262310 1 7.53
CHEMBL441198 1 7.44
CHEMBL430081 1 7.33
CHEMBL385696 1 7.14
CHEMBL407084 1 6.29
CHEMBL262838 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405057 EC50 = 1.24 nM 8.91
CHEMBL412228 EC50 = 3.56 nM 8.45
CHEMBL413832 EC50 = 5.2 nM 8.28
CHEMBL262310 EC50 = 29.4 nM 7.53
CHEMBL441198 EC50 = 36.5 nM 7.44
CHEMBL430081 EC50 = 46.9 nM 7.33
CHEMBL385696 EC50 = 72.4 nM 7.14
CHEMBL407084 EC50 = 515.0 nM 6.29
CHEMBL262838 EC50 = 573.0 nM 6.24