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Assay Detail

CHEMBL755434

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

Functional
Apparent binding affinity of compound was determined by antagonism towards Opioid receptor mu 1 in [35S]GTP-gamma-S, binding assay in guinea pig caudate
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

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
Ki 2 8.04 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610262 1 8.04
CHEMBL611687 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610262 Ki = 9.2 nM 8.04
CHEMBL611687 Ki > 1000.0 nM -