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Assay Detail

CHEMBL680354

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Functional
In vitro inhibitory activity against electrically evoked contractions of guinea pig ileum (GPI)
13
Total Activities
13
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

Potent delta-opioid receptor agonists containing the Dmt-Tic pharmacophore.
Balboni G, Salvadori S, Guerrini R, Negri L, Giannini E, Jinsmaa Y, Bryant SD, Lazarus LH.
J Med Chem (2002) 45 : 5556 -5563
PubMed 12459023 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.78 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278789 DERMORPHIN 1 8.92
CHEMBL606603 1 8.20
CHEMBL109390 1 7.39
CHEMBL607479 1 7.14
CHEMBL607403 1 6.97
CHEMBL607401 1 5.81
CHEMBL442577 1 5.76
CHEMBL607480 1 5.50
CHEMBL607402 1 5.32
CHEMBL26861 1 -
CHEMBL606602 1 -
CHEMBL607481 1 -
CHEMBL606601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278789 DERMORPHIN IC50 = 1.21 nM 8.92
CHEMBL606603 IC50 = 6.36 nM 8.20
CHEMBL109390 IC50 = 40.7 nM 7.39
CHEMBL607479 IC50 = 71.7 nM 7.14
CHEMBL607403 IC50 = 107.5 nM 6.97
CHEMBL607401 IC50 = 1558.0 nM 5.81
CHEMBL442577 IC50 = 1724.0 nM 5.76
CHEMBL607480 IC50 = 3193.0 nM 5.50
CHEMBL607402 IC50 = 4740.0 nM 5.32
CHEMBL26861 IC50 > 1200.0 nM -
CHEMBL606602 IC50 > 10000.0 nM -
CHEMBL607481 IC50 > 10000.0 nM -
CHEMBL606601 IC50 > 10000.0 nM -