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Assay Detail

CHEMBL747873

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

Binding
Binding affinity towards mu opioid receptor was determined in rat brain using [3H]CTOP as radioligand
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
Bartosz-Bechowski H, Davis P, Zalewska T, Slaninova J, Porreca F, Yamamura HI, Hruby VJ.
J Med Chem (1994) 37 : 146 -150
PubMed 8289188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.52 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2372328 1 7.08
CHEMBL2372327 1 6.96
CHEMBL2372329 1 6.75
CHEMBL339320 1 6.55
CHEMBL2372314 1 6.28
CHEMBL31421 1 6.21
CHEMBL2372310 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2372328 IC50 = 83.0 nM 7.08
CHEMBL2372327 IC50 = 110.0 nM 6.96
CHEMBL2372329 IC50 = 180.0 nM 6.75
CHEMBL339320 IC50 = 280.0 nM 6.55
CHEMBL2372314 IC50 = 530.0 nM 6.28
CHEMBL31421 IC50 = 620.0 nM 6.21
CHEMBL2372310 IC50 = 1600.0 nM 5.80