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Assay Detail

CHEMBL3706229

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Binding
Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negative control. HMGR activity under defined assay conditions, containing NADPH and HMG-CoA substrate in a final volume of 0.2 mL of 100 mM potassium phosphatate buffer (120 mM KCI, 1 mM EDTA, 5 mM DTT, pH 7.4), were initiated in the presence or absence (control) of test compounds dissolved in dimethylsulfoxide (DMSO). The rates of NADPH consumption were monitored every 20 seconds, for up to 10 minutes, by spectrophotometer at 37° C. and 340 nm.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A549
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.37 7.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503 LOVASTATIN 4.0 1 7.53
CHEMBL3704922 1 7.44
CHEMBL2347010 1 7.44
CHEMBL3704923 1 7.27
CHEMBL2347011 1 7.27
CHEMBL2347005 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503 LOVASTATIN IC50 = 29.5 nM 7.53
CHEMBL3704922 IC50 = 36.5 nM 7.44
CHEMBL2347010 IC50 = 36.5 nM 7.44
CHEMBL3704923 IC50 = 53.8 nM 7.27
CHEMBL2347011 IC50 = 53.8 nM 7.27
CHEMBL2347005 IC50 = 54.1 nM 7.27