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Assay Detail

CHEMBL753261

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

Functional
The opioid antagonist potency against PL-107 mu-opioid receptor from guinea pig ileum(GPI).Ke (nM) = [antagonist]/(IC50 ratio-1)
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kappa-type opioid receptor (CHEMBL3952)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
Ananthan S, Kezar HS, Carter RL, Saini SK, Rice KC, Wells JL, Davis P, Xu H, Dersch CM, Bilsky EJ, Porreca F, Rothman RB.
J Med Chem (1999) 42 : 3527 -3538
PubMed 10479286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.38 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610522 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610522 Ki = 42.0 nM 7.38