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Assay Detail

CHEMBL1769561

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Functional
Agonist activity at human opioid delta receptor expressed in mouse HN9.10 cells assessed as [35S]GTPgammaS binding
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a potent and efficacious peptide derivative for δ/μ opioid agonist/neurokinin 1 antagonist activity with a 2',6'-dimethyl-L-tyrosine: in vitro, in vivo, and NMR-based structural studies.
Yamamoto T, Nair P, Largent-Milnes TM, Jacobsen NE, Davis P, Ma SW, Yamamura HI, Vanderah TW, Porreca F, Lai J, Hruby VJ.
J Med Chem (2011) 54 : 2029 -2038
PubMed 21366266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 9.18 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766204 2 10.00
CHEMBL1766206 2 9.70
CHEMBL1766207 2 9.24
CHEMBL1766208 2 9.01
CHEMBL200199 BIPHALIN 2 8.96
CHEMBL1766205 2 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766204 EC50 = 0.1 nM 10.00
CHEMBL1766204 EC50 = 0.1259 nM 9.90
CHEMBL1766206 EC50 = 0.2 nM 9.70
CHEMBL1766206 EC50 = 0.4365 nM 9.36
CHEMBL1766207 EC50 = 0.5754 nM 9.24
CHEMBL1766207 EC50 = 0.6 nM 9.22
CHEMBL1766208 EC50 = 0.9772 nM 9.01
CHEMBL1766208 EC50 = 1.0 nM 9.00
CHEMBL200199 BIPHALIN EC50 = 1.1 nM 8.96
CHEMBL200199 BIPHALIN EC50 = 1.122 nM 8.95
CHEMBL1766205 EC50 = 2.3 nM 8.64
CHEMBL1766205 EC50 = 7.079 nM 8.15