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Assay Detail

CHEMBL754564

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

Binding
Inhibitory activity was determined in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor mu 1 in chinese Hamster Ovary (CHO)membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL233)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Neumeyer JL, Zhang A, Xiong W, Gu XH, Hilbert JE, Knapp BI, Negus SS, Mello NK, Bidlack JM.
J Med Chem (2003) 46 : 5162 -5170
PubMed 14613319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.27 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49269 CYCLORPHAN 1 8.77
CHEMBL413512 1 8.74
CHEMBL147511 1 7.80
CHEMBL405131 1 7.05
CHEMBL358104 1 7.05
CHEMBL424328 1 7.00
CHEMBL357334 1 6.89
CHEMBL433697 1 6.77
CHEMBL346436 1 6.44
CHEMBL146756 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49269 CYCLORPHAN IC50 = 1.7 nM 8.77
CHEMBL413512 IC50 = 1.8 nM 8.74
CHEMBL147511 IC50 = 16.0 nM 7.80
CHEMBL405131 IC50 = 90.0 nM 7.05
CHEMBL358104 IC50 = 90.0 nM 7.05
CHEMBL424328 IC50 = 100.0 nM 7.00
CHEMBL357334 IC50 = 130.0 nM 6.89
CHEMBL433697 IC50 = 170.0 nM 6.77
CHEMBL346436 IC50 = 360.0 nM 6.44
CHEMBL146756 IC50 = 610.0 nM 6.21