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Assay Detail

CHEMBL757522

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Functional
Compound was evaluated for the agonistic activity against Opioid receptor mu 1 in guinea pig ileum.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activities of dynorphin A analogues with opioid antagonist properties.
Gairin JE, Mazarguil H, Alvinerie P, Saint-Pierre S, Meunier JC, Cros J.
J Med Chem (1986) 29 : 1913 -1917
PubMed 2876099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.71 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028997 1 9.55
CHEMBL2373009 1 8.55
CHEMBL438223 DYNORPHIN A (1-11) 1 8.54
CHEMBL384584 1 8.48
CHEMBL2373014 1 7.16
CHEMBL3037891 1 6.65
CHEMBL2373012 1 5.05
CHEMBL2373008 1 -
CHEMBL2373013 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028997 IC50 = 0.28 nM 9.55
CHEMBL2373009 IC50 = 2.84 nM 8.55
CHEMBL438223 DYNORPHIN A (1-11) IC50 = 2.88 nM 8.54
CHEMBL384584 IC50 = 3.32 nM 8.48
CHEMBL2373014 IC50 = 69.0 nM 7.16
CHEMBL3037891 IC50 = 222.0 nM 6.65
CHEMBL2373012 IC50 = 8890.0 nM 5.05
CHEMBL2373008 IC50 > 10000.0 nM -
CHEMBL2373013 IC50 > 10000.0 nM -