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Assay Detail

CHEMBL832845

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Functional
Inhibition of Opioid receptor mu 1 in guinea pig ileum assay
18
Total Activities
18
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

Direct influence of C-terminally substituted amino acids in the Dmt-Tic pharmacophore on delta-opioid receptor selectivity and antagonism.
Balboni G, Salvadori S, Guerrini R, Negri L, Giannini E, Bryant SD, Jinsmaa Y, Lazarus LH.
J Med Chem (2004) 47 : 4066 -4071
PubMed 15267245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.45 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085298 1 5.82
CHEMBL3142536 1 5.82
CHEMBL606601 1 5.32
CHEMBL3085297 1 5.18
CHEMBL2371778 1 5.10
CHEMBL607481 1 -
CHEMBL2369980 1 -
CHEMBL2369957 1 -
CHEMBL2369978 1 -
CHEMBL3142535 1 -
CHEMBL2369979 1 -
CHEMBL2371781 1 -
CHEMBL2371782 1 -
CHEMBL2371780 1 -
CHEMBL2371813 1 -
CHEMBL607402 1 -
CHEMBL606602 1 -
CHEMBL2371779 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085298 IC50 = 1500.0 nM 5.82
CHEMBL3142536 IC50 = 1500.0 nM 5.82
CHEMBL606601 IC50 = 4740.0 nM 5.32
CHEMBL3085297 IC50 = 6600.0 nM 5.18
CHEMBL2371778 IC50 = 7870.0 nM 5.10
CHEMBL607481 IC50 > 10000.0 nM -
CHEMBL2369980 IC50 > 10000.0 nM -
CHEMBL2369957 IC50 > 10000.0 nM -
CHEMBL2369978 IC50 > 10000.0 nM -
CHEMBL3142535 IC50 > 10000.0 nM -
CHEMBL2369979 IC50 > 10000.0 nM -
CHEMBL2371781 IC50 > 10000.0 nM -
CHEMBL2371782 IC50 > 10000.0 nM -
CHEMBL2371780 IC50 > 10000.0 nM -
CHEMBL2371813 IC50 > 10000.0 nM -
CHEMBL607402 IC50 > 10000.0 nM -
CHEMBL606602 IC50 > 10000.0 nM -
CHEMBL2371779 IC50 > 10000.0 nM -