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Assay Detail

CHEMBL3584510

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

Functional
Agonist activity at human recombinant delta opioid receptor expressed in CHO cells co-expressing Galphaq66Di5 assessed as stimulation of calcium release by Fluo-4 AM dye-based fluorescence assay
9
Total Activities
9
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 opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Piekielna J, Perlikowska R, do-Rego JC, do-Rego JL, Cerlesi MC, Calo G, Kluczyk A, Łapiński K, Tömböly C, Janecka A.
ACS Med Chem Lett (2015) 6 : 579 -583
PubMed 26005537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.38 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3580749 1 8.06
CHEMBL3580747 1 8.03
CHEMBL31421 1 7.80
CHEMBL411557 DYNORPHIN A (1-17) 1 7.73
CHEMBL3580748 1 7.47
CHEMBL3582487 1 7.29
CHEMBL3580743 1 6.90
CHEMBL3580744 1 6.79
CHEMBL3582484 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3580749 EC50 = 8.71 nM 8.06
CHEMBL3580747 EC50 = 9.333 nM 8.03
CHEMBL31421 EC50 = 15.85 nM 7.80
CHEMBL411557 DYNORPHIN A (1-17) EC50 = 18.62 nM 7.73
CHEMBL3580748 EC50 = 33.88 nM 7.47
CHEMBL3582487 EC50 = 51.29 nM 7.29
CHEMBL3580743 EC50 = 125.89 nM 6.90
CHEMBL3580744 EC50 = 162.18 nM 6.79
CHEMBL3582484 EC50 = 457.09 nM 6.34