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Assay Detail

CHEMBL2330685

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Functional
Agonist activity at human KOR expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis
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 Autocuration

Target

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

Publication

Opioid peptidomimetics: leads for the design of bioavailable mixed efficacy μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands.
Mosberg HI, Yeomans L, Harland AA, Bender AM, Sobczyk-Kojiro K, Anand JP, Clark MJ, Jutkiewicz EM, Traynor JR.
J Med Chem (2013) 56 : 2139 -2149
PubMed 23419026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.72 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322563 1 7.17
CHEMBL2322568 1 6.27
CHEMBL70 MORPHINE 4.0 1 -
CHEMBL2322562 1 -
CHEMBL2322561 1 -
CHEMBL2322560 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322563 EC50 = 68.0 nM 7.17
CHEMBL2322568 EC50 = 540.0 nM 6.27
CHEMBL70 MORPHINE EC50 - -
CHEMBL2322562 EC50 - -
CHEMBL2322561 EC50 - -
CHEMBL2322560 EC50 - -