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Assay Detail

CHEMBL3390812

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

Binding
Inhibition of human HMG-CoA reductase activity using NADPH by spectrophotometrically
6
Total Activities
6
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

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

Publication

Synthesis and highly potent hypolipidemic activity of alpha-asarone- and fibrate-based 2-acyl and 2-alkyl phenols as HMG-CoA reductase inhibitors.
Mendieta A, Jiménez F, Garduño-Siciliano L, Mojica-Villegas A, Rosales-Acosta B, Villa-Tanaca L, Chamorro-Cevallos G, Medina-Franco JL, Meurice N, Gutiérrez RU, Montiel LE, Cruz Mdel C, Tamariz J.
Bioorg Med Chem (2014) 22 : 5871 -5882
PubMed 25311563 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.25 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163691 1 5.32
CHEMBL3344536 1 5.31
CHEMBL333306 TRANS-ASARONE 1 5.23
CHEMBL1163189 1 5.21
CHEMBL1064 SIMVASTATIN 4.0 1 5.21
CHEMBL3344540 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163691 IC50 = 4790.0 nM 5.32
CHEMBL3344536 IC50 = 4940.0 nM 5.31
CHEMBL333306 TRANS-ASARONE IC50 = 5860.0 nM 5.23
CHEMBL1163189 IC50 = 6110.0 nM 5.21
CHEMBL1064 SIMVASTATIN IC50 = 6110.0 nM 5.21
CHEMBL3344540 IC50 = 6430.0 nM 5.19