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Assay Detail

CHEMBL911095

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Functional
Activity at human delta opioid receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
27
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Lee YS, Agnes RS, Davis P, Ma SW, Badghisi H, Lai J, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 165 -168
PubMed 17201419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.95 8.95
EC50 9 7.95 8.96
Emax 9 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 3 8.96
CHEMBL217957 3 8.23
CHEMBL386186 3 8.08
CHEMBL407198 3 8.03
CHEMBL218600 3 7.91
CHEMBL218651 3 7.83
CHEMBL386212 3 7.72
CHEMBL375359 3 7.68
CHEMBL414087 3 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL200199 BIPHALIN IC50 = 1.122 nM 8.95
CHEMBL217957 EC50 = 5.9 nM 8.23
CHEMBL217957 IC50 = 5.888 nM 8.23
CHEMBL386186 EC50 = 8.4 nM 8.08
CHEMBL386186 IC50 = 8.318 nM 8.08
CHEMBL407198 EC50 = 9.4 nM 8.03
CHEMBL407198 IC50 = 9.55 nM 8.02
CHEMBL218600 IC50 = 12.3 nM 7.91
CHEMBL218600 EC50 = 13.0 nM 7.89
CHEMBL218651 IC50 = 14.79 nM 7.83
CHEMBL218651 EC50 = 15.0 nM 7.82
CHEMBL386212 EC50 = 19.0 nM 7.72
CHEMBL386212 IC50 = 19.95 nM 7.70
CHEMBL375359 EC50 = 21.0 nM 7.68
CHEMBL375359 IC50 = 20.89 nM 7.68
CHEMBL414087 EC50 = 74.0 nM 7.13
CHEMBL414087 IC50 = 74.13 nM 7.13
CHEMBL217957 Emax = 120.0 % -
CHEMBL386212 Emax = 89.0 % -
CHEMBL386186 Emax = 93.0 % -
CHEMBL218651 Emax = 64.0 % -
CHEMBL375359 Emax = 48.0 % -
CHEMBL200199 BIPHALIN Emax = 84.0 % -
CHEMBL218600 Emax = 99.0 % -
CHEMBL414087 Emax = 100.0 % -
CHEMBL407198 Emax = 64.0 % -