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Assay Detail

CHEMBL750386

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Functional
Inhibitory concentration required for 50 percent inhibition of opioid receptor delta 1 induced contractions in mouse vas deferens (MVD) smooth muscle contraction assays
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Identification of opioid ligands possessing mixed micro agonist/delta antagonist activity among pyridomorphinans derived from naloxone, oxymorphone, and hydromorphone [correction of hydropmorphone].
Ananthan S, Khare NK, Saini SK, Seitz LE, Bartlett JL, Davis P, Dersch CM, Porreca F, Rothman RB, Bilsky EJ.
J Med Chem (2004) 47 : 1400 -1412
PubMed 14998329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.89 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31421 1 8.24
CHEMBL611432 1 7.32
CHEMBL611687 1 6.82
CHEMBL611434 1 6.67
CHEMBL283287 1 6.61
CHEMBL611437 1 6.31
CHEMBL611688 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31421 IC50 = 5.81 nM 8.24
CHEMBL611432 IC50 = 48.4 nM 7.32
CHEMBL611687 IC50 = 152.0 nM 6.82
CHEMBL611434 IC50 = 213.0 nM 6.67
CHEMBL283287 IC50 = 243.0 nM 6.61
CHEMBL611437 IC50 = 489.0 nM 6.31
CHEMBL611688 IC50 = 565.0 nM 6.25