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Assay Detail

CHEMBL991179

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

Binding
Inhibition of human HMGCoA reductase
13
Total Activities
12
Compounds Tested
2
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

Novel Acetylenic Acids from the Root Bark of Paramacrolobium caeruleum: Inhibitors of 3-Hydroxy-3-methyl-glutaryl Coenzyme A Reductase
Patil AD, Chan JA, Lois-Flamberg P, Mayer RJ, Westley JW
J Nat Prod (1989) 52 : 153 -161
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.86 8.70
Ki 1 9.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503 LOVASTATIN 4.0 2 9.22
CHEMBL489540 1 6.30
CHEMBL504781 1 5.82
CHEMBL482803 1 5.70
CHEMBL482601 1 5.52
CHEMBL501307 1 5.52
CHEMBL485858 1 5.30
CHEMBL482804 1 5.30
CHEMBL483819 1 5.30
CHEMBL448462 1 5.16
CHEMBL46403 STEARIC ACID -1.0 1 -
CHEMBL8659 OLEIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503 LOVASTATIN Ki = 0.6 nM 9.22
CHEMBL503 LOVASTATIN IC50 = 2.0 nM 8.70
CHEMBL489540 IC50 = 500.0 nM 6.30
CHEMBL504781 IC50 = 1500.0 nM 5.82
CHEMBL482803 IC50 = 2000.0 nM 5.70
CHEMBL482601 IC50 = 3000.0 nM 5.52
CHEMBL501307 IC50 = 3000.0 nM 5.52
CHEMBL485858 IC50 = 5000.0 nM 5.30
CHEMBL482804 IC50 = 5000.0 nM 5.30
CHEMBL483819 IC50 = 5000.0 nM 5.30
CHEMBL448462 IC50 = 7000.0 nM 5.16
CHEMBL46403 STEARIC ACID IC50 - -
CHEMBL8659 OLEIC ACID IC50 - -