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Assay Detail

CHEMBL753435

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

Binding
Inhibitory activity against opioid receptor mu of guinea pig brain using [3H]DAGO radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, opioid receptor binding profile, and antinociceptive activity of 1-azaspiro[4.5]decan-10-yl amides.
Fujimoto RA, Boxer J, Jackson RH, Simke JP, Neale RF, Snowhill EW, Barbaz BJ, Williams M, Sills MA.
J Med Chem (1989) 32 : 1259 -1265
PubMed 2542556 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.27 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592 LEVORPHANOL 4.0 1 9.22
CHEMBL279065 1 8.70
CHEMBL22211 1 8.20
CHEMBL553991 1 7.92
CHEMBL553782 1 7.80
CHEMBL553062 1 7.77
CHEMBL277202 1 7.68
CHEMBL23016 1 6.82
CHEMBL282244 1 6.68
CHEMBL22569 1 6.66
CHEMBL539228 1 6.26
CHEMBL22458 1 6.24
CHEMBL542069 1 6.22
CHEMBL542564 1 5.66
CHEMBL25386 1 -
CHEMBL544684 1 -
CHEMBL23777 1 -
CHEMBL554212 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592 LEVORPHANOL IC50 = 0.6 nM 9.22
CHEMBL279065 IC50 = 2.0 nM 8.70
CHEMBL22211 IC50 = 6.3 nM 8.20
CHEMBL553991 IC50 = 12.0 nM 7.92
CHEMBL553782 IC50 = 16.0 nM 7.80
CHEMBL553062 IC50 = 17.0 nM 7.77
CHEMBL277202 IC50 = 21.0 nM 7.68
CHEMBL23016 IC50 = 150.0 nM 6.82
CHEMBL282244 IC50 = 210.0 nM 6.68
CHEMBL22569 IC50 = 220.0 nM 6.66
CHEMBL539228 IC50 = 550.0 nM 6.26
CHEMBL22458 IC50 = 580.0 nM 6.24
CHEMBL542069 IC50 = 600.0 nM 6.22
CHEMBL542564 IC50 = 2200.0 nM 5.66
CHEMBL25386 IC50 > 10000.0 nM -
CHEMBL544684 IC50 > 10000.0 nM -
CHEMBL23777 IC50 > 10000.0 nM -
CHEMBL554212 IC50 > 10000.0 nM -