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Assay Detail

CHEMBL746594

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

Functional
Inhibition of contraction (agonistic activity) of mouse vas deferens (MVD) at 1 uM concentration.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Expert

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

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
IC50 11 8.72 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118487 1 8.92
CHEMBL2112575 1 8.52
CHEMBL567175 NALTRINDOLE 1 -
CHEMBL610261 1 -
CHEMBL610522 1 -
CHEMBL118479 1 -
CHEMBL2112568 1 -
CHEMBL2112570 1 -
CHEMBL2112576 1 -
CHEMBL2112572 1 -
CHEMBL2112571 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118487 IC50 = 1.2 nM 8.92
CHEMBL2112575 IC50 = 3.0 nM 8.52
CHEMBL567175 NALTRINDOLE IC50 = 16.0 % -
CHEMBL610261 IC50 = 21.0 % -
CHEMBL610522 IC50 = 4.7 % -
CHEMBL118479 IC50 = 31.0 % -
CHEMBL2112568 IC50 = - % -
CHEMBL2112570 IC50 = 15.4 % -
CHEMBL2112576 IC50 = - % -
CHEMBL2112572 IC50 = - % -
CHEMBL2112571 IC50 = - % -