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Assay Detail

CHEMBL4684606

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Functional
Agonist activity at human kappa opioid receptor expressed in CHO cells incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method
5
Total Activities
5
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

Discovery of 3-((dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)-N-phenylpiperidine-1-carboxamide as novel potent analgesic.
Huang H,Wang W,Xu X,Zhu C,Wang Y,Liu J,Li W,Fu W
Eur J Med Chem (2020) 189 : 112070 -112070
PubMed 31982651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.76 8.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290543 1 8.56
CHEMBL4786173 1 6.96
CHEMBL38874 DAMGO 1 -
CHEMBL31421 1 -
CHEMBL1400 O-DESMETHYL TRAMADOL 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290543 EC50 = 2.77 nM 8.56
CHEMBL4786173 EC50 = 110.4 nM 6.96
CHEMBL38874 DAMGO EC50 - -
CHEMBL31421 EC50 - -
CHEMBL1400 O-DESMETHYL TRAMADOL EC50 - -