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Assay Detail

CHEMBL4669980

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

Binding
Inhibition of recombinant human ACC2 using acetyl coA as substrate incubated for 1 hr by transcreener fluorescence polarization assay
ChEMBL ↗
18
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetyl-CoA carboxylase 2 (CHEMBL4829) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 18 7.29 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4753907 — — 2 8.30
CHEMBL4762472 — — 2 8.03
CHEMBL4743101 — — 2 7.90
CHEMBL4567446 CLESACOSTAT 2.0 2 7.60
CHEMBL4759617 — — 2 7.50
CHEMBL4777931 — — 2 7.04
CHEMBL4799861 — — 2 6.72
CHEMBL4785069 — — 2 6.70
CHEMBL4744660 — — 2 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4753907 — IC50 = 5.012 nM 8.30
CHEMBL4753907 — IC50 = 5.6 nM 8.25
CHEMBL4762472 — IC50 = 9.4 nM 8.03
CHEMBL4762472 — IC50 = 10.0 nM 8.00
CHEMBL4743101 — IC50 = 12.59 nM 7.90
CHEMBL4743101 — IC50 = 13.0 nM 7.89
CHEMBL4567446 CLESACOSTAT IC50 = 25.12 nM 7.60
CHEMBL4567446 CLESACOSTAT IC50 = 26.0 nM 7.58
CHEMBL4759617 — IC50 = 31.62 nM 7.50
CHEMBL4759617 — IC50 = 33.0 nM 7.48
CHEMBL4777931 — IC50 = 92.0 nM 7.04
CHEMBL4777931 — IC50 = 100.0 nM 7.00
CHEMBL4799861 — IC50 = 190.0 nM 6.72
CHEMBL4785069 — IC50 = 199.53 nM 6.70
CHEMBL4799861 — IC50 = 199.53 nM 6.70
CHEMBL4785069 — IC50 = 200.0 nM 6.70
CHEMBL4744660 — IC50 = 1200.0 nM 5.92
CHEMBL4744660 — IC50 = 1258.93 nM 5.90