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Assay Detail

CHEMBL942701

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Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 5. Opioid receptor binding properties of N-((4'-phenyl)-phenethyl) analogues of 8-CAC.
VanAlstine MA, Wentland MP, Cohen DJ, Bidlack JM.
Bioorg Med Chem Lett (2007) 17 : 6516 -6520
PubMed 17935988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 8.29 9.17
Emax 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL249985 2 9.17
CHEMBL438871 2 8.70
CHEMBL377789 2 8.52
CHEMBL13470 SNC-80 2 8.32
CHEMBL250993 2 7.85
CHEMBL401278 2 7.75
CHEMBL249567 2 7.70
CHEMBL430397 2 -
CHEMBL399465 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL249985 EC50 = 0.68 nM 9.17
CHEMBL438871 EC50 = 2.0 nM 8.70
CHEMBL377789 EC50 = 3.0 nM 8.52
CHEMBL13470 SNC-80 EC50 = 4.8 nM 8.32
CHEMBL250993 EC50 = 14.0 nM 7.85
CHEMBL401278 EC50 = 18.0 nM 7.75
CHEMBL249567 EC50 = 20.0 nM 7.70
CHEMBL377789 Emax = 69.0 % -
CHEMBL13470 SNC-80 Emax = 120.0 % -
CHEMBL430397 EC50 - -
CHEMBL430397 Emax - -
CHEMBL438871 Emax = 45.0 % -
CHEMBL250993 Emax = 85.0 % -
CHEMBL249567 Emax = 120.0 % -
CHEMBL399465 EC50 - -
CHEMBL399465 Emax - -
CHEMBL401278 Emax = 43.0 % -
CHEMBL249985 Emax = 70.0 % -