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Assay Detail

CHEMBL884714

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

Binding
Binding to mu opioid receptor by using [3H]DAMGO as radioligand in guinea pig brain minus cerebellum
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Mu-type opioid receptor (CHEMBL4354)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Palladium-catalyzed synthesis of C3-substituted 3-deoxymorphines.
Hedberg MH, Johansson AM, Fowler CJ, Terenius L, Hacksell U
Bioorg Med Chem Lett (1994) 4 : 2527 -2532
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.11 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70 MORPHINE 4.0 1 8.07
CHEMBL87247 1 6.70
CHEMBL85457 1 6.28
CHEMBL82576 1 6.19
CHEMBL84484 1 5.58
CHEMBL442709 1 5.48
CHEMBL85089 1 5.35
CHEMBL440694 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70 MORPHINE IC50 = 8.5 nM 8.07
CHEMBL87247 IC50 = 200.0 nM 6.70
CHEMBL85457 IC50 = 530.0 nM 6.28
CHEMBL82576 IC50 = 640.0 nM 6.19
CHEMBL84484 IC50 = 2600.0 nM 5.58
CHEMBL442709 IC50 = 3300.0 nM 5.48
CHEMBL85089 IC50 = 4500.0 nM 5.35
CHEMBL440694 IC50 = 6400.0 nM 5.19