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Assay Detail

CHEMBL900982

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Functional
Agonist activity at human delta-opioid receptor expressed in CHO cells after 90 mins by [35S]GTP-gamma-S assay
16
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 Intermediate

Target

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

Publication

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Lee YS, Petrov R, Park CK, Ma SW, Davis P, Lai J, Porreca F, Vardanyan R, Hruby VJ.
J Med Chem (2007) 50 : 5528 -5532
PubMed 17927164 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 7.21 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235109 2 9.12
CHEMBL235107 2 7.54
CHEMBL392207 2 7.43
CHEMBL392206 2 6.96
CHEMBL439026 2 6.82
CHEMBL392185 2 6.78
CHEMBL235743 2 6.72
CHEMBL235106 2 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235109 EC50 = 0.7586 nM 9.12
CHEMBL235109 EC50 = 0.77 nM 9.11
CHEMBL235107 EC50 = 28.84 nM 7.54
CHEMBL235107 EC50 = 29.0 nM 7.54
CHEMBL392207 EC50 = 37.15 nM 7.43
CHEMBL392207 EC50 = 37.0 nM 7.43
CHEMBL392206 EC50 = 110.0 nM 6.96
CHEMBL392206 EC50 = 112.2 nM 6.95
CHEMBL439026 EC50 = 151.36 nM 6.82
CHEMBL439026 EC50 = 150.0 nM 6.82
CHEMBL392185 EC50 = 165.96 nM 6.78
CHEMBL392185 EC50 = 170.0 nM 6.77
CHEMBL235743 EC50 = 190.55 nM 6.72
CHEMBL235743 EC50 = 190.0 nM 6.72
CHEMBL235106 EC50 = 512.86 nM 6.29
CHEMBL235106 EC50 = 510.0 nM 6.29