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Assay Detail

CHEMBL751659

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibitory concentration required for 50% inhibition of antagonism towards opioid receptor delta 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Delta-type opioid receptor (CHEMBL236)
Type SINGLE PROTEIN
Organism Homo sapiens

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 3 6.81 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611431 1 7.26
CHEMBL611437 1 7.13
CHEMBL611434 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611431 IC50 = 55.0 nM 7.26
CHEMBL611437 IC50 = 74.0 nM 7.13
CHEMBL611434 IC50 = 920.0 nM 6.04