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Assay Detail

CHEMBL758124

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

Functional
Agonistic activity towards Opioid receptor mu 1 was determined in [35S]GTP-gamma-S, binding assay in guinea pig caudate
5
Total Activities
5
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
EC50 5 5.74 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611434 1 6.18
CHEMBL611435 1 5.52
CHEMBL611687 1 5.52
CHEMBL611432 1 -
CHEMBL38874 DAMGO 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611434 EC50 = 660.0 nM 6.18
CHEMBL611435 EC50 = 3000.0 nM 5.52
CHEMBL611687 EC50 = 3000.0 nM 5.52
CHEMBL611432 EC50 - nM -
CHEMBL38874 DAMGO EC50 = 414.0 -