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Assay Detail

CHEMBL4669878

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

Functional
Inhibition of DNL in po dosed Sprague-Dawley rat assessed as reduction in DNL level in liver pretreated with one hr followed by [14C]-acetate treatment and measured after 1 hr
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.
Huard K,Smith AC,Cappon G,Dow RL,Edmonds DJ,El-Kattan A,Esler WP,Fernando DP,Griffith DA,Kalgutkar AS,Ross TT,Bagley SW,Beebe D,Bi YA,Cabral S,Crowley C,Doran SD,Dowling MS,Liras S,Mascitti V,Niosi M,Pfefferkorn JA,Polivkova J,Préville C,Price DA,Shavnya A,Shirai N,Smith AH,Southers JR,Tess DA,Thuma BA,Varma MV,Yang X
J Med Chem (2020) 63 : 10879 -10896
PubMed 32809824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 1 - -
EC50 1 8.27 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4567446 CLESACOSTAT 2.0 2 8.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4567446 CLESACOSTAT EC50 = 5.4 nM 8.27
CHEMBL4567446 CLESACOSTAT Inhibition - % -