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Assay Detail

CHEMBL911093

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

Binding
Displacement of [3H]DPDPE from human delta opioid receptor expressed in HN9.10 cells
16
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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 8 8.23 8.86
Ki 8 8.59 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL217957 2 9.20
CHEMBL375359 2 9.10
CHEMBL386212 2 8.96
CHEMBL407198 2 8.85
CHEMBL218651 2 8.66
CHEMBL218600 2 8.41
CHEMBL386186 2 8.16
CHEMBL414087 2 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL217957 Ki = 0.63 nM 9.20
CHEMBL375359 Ki = 0.8 nM 9.10
CHEMBL386212 Ki = 1.1 nM 8.96
CHEMBL217957 IC50 = 1.38 nM 8.86
CHEMBL407198 Ki = 1.4 nM 8.85
CHEMBL375359 IC50 = 1.66 nM 8.78
CHEMBL218651 Ki = 2.2 nM 8.66
CHEMBL386212 IC50 = 2.57 nM 8.59
CHEMBL407198 IC50 = 3.236 nM 8.49
CHEMBL218600 Ki = 3.9 nM 8.41
CHEMBL218651 IC50 = 5.129 nM 8.29
CHEMBL386186 Ki = 6.9 nM 8.16
CHEMBL218600 IC50 = 9.12 nM 8.04
CHEMBL386186 IC50 = 16.22 nM 7.79
CHEMBL414087 Ki = 45.0 nM 7.35
CHEMBL414087 IC50 = 93.33 nM 7.03