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Assay Detail

CHEMBL4136380

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Functional
Agonist activity at delta-type opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated contractions
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Delta-type opioid receptor (CHEMBL3222)
Type SINGLE PROTEIN
Organism Mus musculus

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 9 8.15 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1782140 1 9.38
CHEMBL4173234 1 9.07
CHEMBL4166388 1 8.96
CHEMBL4165323 1 8.85
CHEMBL4164236 1 8.07
CHEMBL278789 DERMORPHIN 1 7.75
CHEMBL4172559 1 7.33
CHEMBL4174890 1 7.04
CHEMBL4161890 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1782140 IC50 = 0.42 nM 9.38
CHEMBL4173234 IC50 = 0.86 nM 9.07
CHEMBL4166388 IC50 = 1.09 nM 8.96
CHEMBL4165323 IC50 = 1.42 nM 8.85
CHEMBL4164236 IC50 = 8.51 nM 8.07
CHEMBL278789 DERMORPHIN IC50 = 17.8 nM 7.75
CHEMBL4172559 IC50 = 47.1 nM 7.33
CHEMBL4174890 IC50 = 90.5 nM 7.04
CHEMBL4161890 IC50 = 114.0 nM 6.94