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Assay Detail

CHEMBL3787925

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Functional
Agonist activity at human delta opioid receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
8
Total Activities
8
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 and evaluation of novel opioid ligands with a C-homomorphinan skeleton.
Ishikawa K, Mochizuki Y, Hirayama S, Nemoto T, Nagai K, Itoh K, Fujii H.
Bioorg Med Chem (2016) 24 : 2199 -2205
PubMed 27079125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.60 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3787263 1 9.09
CHEMBL3787016 1 8.97
CHEMBL3785854 1 8.85
CHEMBL3786083 1 8.74
CHEMBL3785265 1 8.50
CHEMBL3787663 1 8.13
CHEMBL3786970 1 7.90
CHEMBL3786218 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3787263 EC50 = 0.813 nM 9.09
CHEMBL3787016 EC50 = 1.06 nM 8.97
CHEMBL3785854 EC50 = 1.4 nM 8.85
CHEMBL3786083 EC50 = 1.83 nM 8.74
CHEMBL3785265 EC50 = 3.17 nM 8.50
CHEMBL3787663 EC50 = 7.32 nM 8.13
CHEMBL3786970 EC50 = 12.5 nM 7.90
CHEMBL3786218 EC50 > 10000.0 nM -