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Assay Detail

CHEMBL4136379

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Functional
Agonist activity at mu-opioid receptor in guinea pig ileum assessed as inhibition of electrically induced contractions
9
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

χ-Space Screening of Dermorphin-Based Tetrapeptides through Use of Constrained Arylazepinone and Quinolinone Scaffolds.
Van der Poorten O, Van Den Hauwe R, Eiselt E, Betti C, Guillemyn K, Chung NN, Hallé F, Bihel F, Schiller PW, Tourwé D, Sarret P, Gendron L, Ballet S.
ACS Med Chem Lett (2017) 8 : 1177 -1182
PubMed 29152051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.76 9.60
IC25 1 - -
IC35 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4165323 1 9.60
CHEMBL1782140 1 9.49
CHEMBL4166388 1 9.37
CHEMBL278789 DERMORPHIN 1 8.97
CHEMBL4173234 1 8.95
CHEMBL4161890 1 7.67
CHEMBL4172559 1 7.30
CHEMBL4164236 1 -
CHEMBL4174890 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4165323 IC50 = 0.252 nM 9.60
CHEMBL1782140 IC50 = 0.32 nM 9.49
CHEMBL4166388 IC50 = 0.43 nM 9.37
CHEMBL278789 DERMORPHIN IC50 = 1.06 nM 8.97
CHEMBL4173234 IC50 = 1.13 nM 8.95
CHEMBL4161890 IC50 = 21.4 nM 7.67
CHEMBL4172559 IC50 = 50.4 nM 7.30
CHEMBL4164236 IC25 = 22.0 nM -
CHEMBL4174890 IC35 = 33.7 nM -