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Assay Detail

CHEMBL842476

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

Binding
Binding affinity towards mu opioid receptor using [3H]- -DAMGO (1.5 nM) as radioligand in rat brain membranes
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Brain membranes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL270)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.
Cottney J, Rankovic Z, Morphy JR.
Bioorg Med Chem Lett (1999) 9 : 1323 -1328
PubMed 10340622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.31 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL280801 1 6.42
CHEMBL611163 1 5.44
CHEMBL13470 SNC-80 1 5.32
CHEMBL611161 1 5.20
CHEMBL611165 1 5.19
CHEMBL611160 1 5.19
CHEMBL28337 1 4.38
CHEMBL283335 1 -
CHEMBL24035 2 -
CHEMBL283466 1 -
CHEMBL1169547 1 -
CHEMBL2374437 1 -
CHEMBL24569 1 -
CHEMBL611162 1 -
CHEMBL262634 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL280801 IC50 = 380.0 nM 6.42
CHEMBL611163 IC50 = 3600.0 nM 5.44
CHEMBL13470 SNC-80 IC50 = 4800.0 nM 5.32
CHEMBL611161 IC50 = 6300.0 nM 5.20
CHEMBL611165 IC50 = 6400.0 nM 5.19
CHEMBL611160 IC50 = 6500.0 nM 5.19
CHEMBL28337 IC50 = 41600.0 nM 4.38
CHEMBL283335 IC50 > 50000.0 nM -
CHEMBL24035 IC50 > 10000.0 nM -
CHEMBL283466 IC50 > 10000.0 nM -
CHEMBL1169547 IC50 > 10000.0 nM -
CHEMBL2374437 IC50 > 10000.0 nM -
CHEMBL24035 IC50 > 10000.0 nM -
CHEMBL24569 IC50 > 10000.0 nM -
CHEMBL611162 IC50 > 10000.0 nM -
CHEMBL262634 IC50 > 21600.0 nM -