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Assay Detail

CHEMBL756175

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Binding
Compound was evaluated for binding affinity towards Opioid receptor delta 1 by displacing 125 I-deltorphin II
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel Dmt-Tic dipeptide analogues as selective delta-opioid receptor antagonists.
Pagé D, McClory A, Mischki T, Schmidt R, Butterworth J, St-Onge S, Labarre M, Payza K, Brown W.
Bioorg Med Chem Lett (2000) 10 : 167 -170
PubMed 10673103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.30 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571492 1 8.80
CHEMBL2114981 1 8.60
CHEMBL2114978 1 8.42
CHEMBL48098 1 8.31
CHEMBL2114977 1 8.24
CHEMBL297452 1 7.96
CHEMBL2114982 1 7.92
CHEMBL2114980 1 7.88
CHEMBL418080 1 7.87
CHEMBL46160 1 7.28
CHEMBL2115427 1 7.09
CHEMBL2115429 1 6.91
CHEMBL44732 1 6.63
CHEMBL2115430 1 6.24
CHEMBL2114986 1 5.97
CHEMBL47564 1 5.94
CHEMBL45842 1 5.82
CHEMBL430777 1 5.59
CHEMBL2115434 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571492 IC50 = 1.6 nM 8.80
CHEMBL2114981 IC50 = 2.5 nM 8.60
CHEMBL2114978 IC50 = 3.8 nM 8.42
CHEMBL48098 IC50 = 4.9 nM 8.31
CHEMBL2114977 IC50 = 5.8 nM 8.24
CHEMBL297452 IC50 = 10.9 nM 7.96
CHEMBL2114982 IC50 = 12.1 nM 7.92
CHEMBL2114980 IC50 = 13.2 nM 7.88
CHEMBL418080 IC50 = 13.5 nM 7.87
CHEMBL46160 IC50 = 52.7 nM 7.28
CHEMBL2115427 IC50 = 81.7 nM 7.09
CHEMBL2115429 IC50 = 122.0 nM 6.91
CHEMBL44732 IC50 = 236.0 nM 6.63
CHEMBL2115430 IC50 = 571.0 nM 6.24
CHEMBL2114986 IC50 = 1080.0 nM 5.97
CHEMBL47564 IC50 = 1160.0 nM 5.94
CHEMBL45842 IC50 = 1520.0 nM 5.82
CHEMBL430777 IC50 = 2540.0 nM 5.59
CHEMBL2115434 IC50 > 10000.0 nM -