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Assay Detail

CHEMBL3762661

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Functional
Agonist activity at human recombinant DOR expressed in CHO cells assessed as calcium mobilization by Fluo-4 AM based fluorescence analysis
4
Total Activities
4
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

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of mixed MOR/KOR efficacy cyclic opioid peptide analogs with antinociceptive activity after systemic administration.
Perlikowska R, Piekielna J, Gentilucci L, De Marco R, Cerlesi MC, Calo G, Artali R, Tömböly C, Kluczyk A, Janecka A.
Eur J Med Chem (2016) 109 : 276 -286
PubMed 26785295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.44 7.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A 1 7.73
CHEMBL31421 1 7.57
CHEMBL3759179 1 7.27
CHEMBL3759167 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL405618 ANALOG OF DYNORPHIN A EC50 = 18.62 nM 7.73
CHEMBL31421 EC50 = 26.92 nM 7.57
CHEMBL3759179 EC50 = 53.7 nM 7.27
CHEMBL3759167 EC50 = 64.57 nM 7.19