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Assay Detail

CHEMBL747922

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

Binding
In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
Cheng CY, Hsin LW, Tsai MC, Schmidt WK, Smith C, Tam SW.
J Med Chem (1994) 37 : 3121 -3127
PubMed 7932535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.30 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106027 1 9.60
CHEMBL104042 1 9.24
CHEMBL80 NALOXONE 4.0 1 8.96
CHEMBL319236 1 8.85
CHEMBL323281 1 8.41
CHEMBL324418 1 8.11
CHEMBL106910 1 7.72
CHEMBL106085 1 7.54
CHEMBL70 MORPHINE 4.0 1 7.42
CHEMBL321289 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106027 Ki = 0.25 nM 9.60
CHEMBL104042 Ki = 0.57 nM 9.24
CHEMBL80 NALOXONE Ki = 1.1 nM 8.96
CHEMBL319236 Ki = 1.4 nM 8.85
CHEMBL323281 Ki = 3.9 nM 8.41
CHEMBL324418 Ki = 7.8 nM 8.11
CHEMBL106910 Ki = 19.0 nM 7.72
CHEMBL106085 Ki = 29.0 nM 7.54
CHEMBL70 MORPHINE Ki = 38.0 nM 7.42
CHEMBL321289 Ki = 76.0 nM 7.12