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Assay Detail

CHEMBL757307

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Binding
Compound was evaluated for binding affinity towards Opioid receptor mu 1 by displacing 125 I-FK-33824
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

Mu-type opioid receptor (CHEMBL233)
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 5.73 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418080 1 6.85
CHEMBL2114978 1 6.23
CHEMBL2114980 1 6.20
CHEMBL571492 1 6.05
CHEMBL2114977 1 5.94
CHEMBL2114986 1 5.91
CHEMBL2114981 1 5.78
CHEMBL2115429 1 5.71
CHEMBL44732 1 5.67
CHEMBL297452 1 5.64
CHEMBL46160 1 5.61
CHEMBL48098 1 5.58
CHEMBL2114982 1 5.54
CHEMBL45842 1 5.33
CHEMBL47564 1 5.14
CHEMBL2115434 1 5.09
CHEMBL2115430 1 5.08
CHEMBL430777 1 -
CHEMBL2115427 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418080 IC50 = 142.0 nM 6.85
CHEMBL2114978 IC50 = 587.0 nM 6.23
CHEMBL2114980 IC50 = 635.0 nM 6.20
CHEMBL571492 IC50 = 894.0 nM 6.05
CHEMBL2114977 IC50 = 1140.0 nM 5.94
CHEMBL2114986 IC50 = 1240.0 nM 5.91
CHEMBL2114981 IC50 = 1670.0 nM 5.78
CHEMBL2115429 IC50 = 1940.0 nM 5.71
CHEMBL44732 IC50 = 2160.0 nM 5.67
CHEMBL297452 IC50 = 2280.0 nM 5.64
CHEMBL46160 IC50 = 2440.0 nM 5.61
CHEMBL48098 IC50 = 2650.0 nM 5.58
CHEMBL2114982 IC50 = 2870.0 nM 5.54
CHEMBL45842 IC50 = 4640.0 nM 5.33
CHEMBL47564 IC50 = 7220.0 nM 5.14
CHEMBL2115434 IC50 = 8130.0 nM 5.09
CHEMBL2115430 IC50 = 8240.0 nM 5.08
CHEMBL430777 IC50 > 10000.0 nM -
CHEMBL2115427 IC50 - nM -