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Assay Detail

CHEMBL911101

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Functional
Activity at mu opioid receptor assessed as contraction of electrically-stimulated Hartley 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 Expert

Target

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

Publication

Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
Lee YS, Agnes RS, Davis P, Ma SW, Badghisi H, Lai J, Porreca F, Hruby VJ.
J Med Chem (2007) 50 : 165 -168
PubMed 17201419 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.91 8.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200199 BIPHALIN 1 8.06
CHEMBL218651 1 7.12
CHEMBL407198 1 7.09
CHEMBL386212 1 7.03
CHEMBL375359 1 7.01
CHEMBL386186 1 6.68
CHEMBL217957 1 6.62
CHEMBL414087 1 6.34
CHEMBL218600 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200199 BIPHALIN IC50 = 8.8 nM 8.06
CHEMBL218651 IC50 = 76.0 nM 7.12
CHEMBL407198 IC50 = 81.0 nM 7.09
CHEMBL386212 IC50 = 93.0 nM 7.03
CHEMBL375359 IC50 = 97.0 nM 7.01
CHEMBL386186 IC50 = 210.0 nM 6.68
CHEMBL217957 IC50 = 240.0 nM 6.62
CHEMBL414087 IC50 = 460.0 nM 6.34
CHEMBL218600 IC50 = 530.0 nM 6.28