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Assay Detail

CHEMBL893760

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

Binding
Displacement of [3H]DAGO from mu opioid receptor in rat brain membrane
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Differential receptor binding characteristics of consecutive phenylalanines in micro-opioid specific peptide ligand endomorphin-2.
Honda T, Shirasu N, Isozaki K, Kawano M, Shigehiro D, Chuman Y, Fujita T, Nose T, Shimohigashi Y.
Bioorg Med Chem (2007) 15 : 3883 -3888
PubMed 17395470 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.99 8.95

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38874 DAMGO 1 8.95
CHEMBL316446 ENDOMORPHIN-1 1 8.72
CHEMBL242980 1 8.56
CHEMBL333357 ENDOMORPHIN 2 1 8.46
CHEMBL397448 1 7.93
CHEMBL243200 1 7.47
CHEMBL242981 1 7.21
CHEMBL242984 1 7.21
CHEMBL390914 1 7.12
CHEMBL388265 1 7.07
CHEMBL364703 1 7.06
CHEMBL243201 1 6.86
CHEMBL223552 1 6.83
CHEMBL438833 1 6.64
CHEMBL1161991 1 6.39
CHEMBL242979 1 6.04
CHEMBL242089 1 6.03
CHEMBL242974 1 5.96
CHEMBL242087 1 5.58
CHEMBL387816 1 5.42
CHEMBL242330 1 5.35
CHEMBL1161990 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38874 DAMGO IC50 = 1.13 nM 8.95
CHEMBL316446 ENDOMORPHIN-1 IC50 = 1.89 nM 8.72
CHEMBL242980 IC50 = 2.74 nM 8.56
CHEMBL333357 ENDOMORPHIN 2 IC50 = 3.46 nM 8.46
CHEMBL397448 IC50 = 11.7 nM 7.93
CHEMBL243200 IC50 = 33.9 nM 7.47
CHEMBL242981 IC50 = 62.2 nM 7.21
CHEMBL242984 IC50 = 62.0 nM 7.21
CHEMBL390914 IC50 = 76.5 nM 7.12
CHEMBL388265 IC50 = 85.4 nM 7.07
CHEMBL364703 IC50 = 87.1 nM 7.06
CHEMBL243201 IC50 = 138.0 nM 6.86
CHEMBL223552 IC50 = 148.0 nM 6.83
CHEMBL438833 IC50 = 230.0 nM 6.64
CHEMBL1161991 IC50 = 408.0 nM 6.39
CHEMBL242979 IC50 = 917.0 nM 6.04
CHEMBL242089 IC50 = 926.0 nM 6.03
CHEMBL242974 IC50 = 1100.0 nM 5.96
CHEMBL242087 IC50 = 2650.0 nM 5.58
CHEMBL387816 IC50 = 3810.0 nM 5.42
CHEMBL242330 IC50 = 4490.0 nM 5.35
CHEMBL1161990 IC50 > 1000000.0 nM -