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Assay Detail

CHEMBL753317

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Functional
Inhibition of forskolin-stimulated adenylyl cyclase activity by compound in CHO cells expressing Opioid receptor kappa 1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
Vig BS, Murray TF, Aldrich JV.
J Med Chem (2004) 47 : 446 -455
PubMed 14711314 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.50 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411282 1 9.41
CHEMBL439272 1 9.27
CHEMBL261992 1 9.19
CHEMBL414904 1 8.38
CHEMBL405307 1 7.92
CHEMBL438044 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411282 EC50 = 0.39 nM 9.41
CHEMBL439272 EC50 = 0.54 nM 9.27
CHEMBL261992 EC50 = 0.65 nM 9.19
CHEMBL414904 EC50 = 4.19 nM 8.38
CHEMBL405307 EC50 = 12.0 nM 7.92
CHEMBL438044 EC50 = 153.0 nM 6.82