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ChEMBL

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ChEMBL Statistics
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Target Report Card

Target Name and Classification

Target ID CHEMBL402
Target Type SINGLE PROTEIN
Preferred Name HMG-CoA reductase
Synonyms 3-hydroxy-3-methylglutaryl-coenzyme A reductase | HMG-CoA reductase | HMGCR
Organism Homo sapiens
Species Group No
Protein Target Classification
  • enzyme > oxidoreductase

Target Components

Component Description Relationship Accession
3-hydroxy-3-methylglutaryl-coenzyme A reductase SINGLE PROTEIN P04035

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL503 LOVASTATIN HMG-CoA reductase inhibitor 4 DailyMed
CHEMBL690 PRAVASTATIN SODIUM HMG-CoA reductase inhibitor 4 DailyMed
CHEMBL1064 SIMVASTATIN HMG-CoA reductase inhibitor 4 DailyMed
CHEMBL393220 ATORVASTATIN CALCIUM HMG-CoA reductase inhibitor 4 DailyMed
CHEMBL1200563 CERIVASTATIN SODIUM HMG-CoA reductase inhibitor 4 ISBN
CHEMBL1237061 PITAVASTATIN CALCIUM HMG-CoA reductase inhibitor 4 DailyMed FDA
CHEMBL1744447 ROSUVASTATIN CALCIUM HMG-CoA reductase inhibitor 4 DailyMed
CHEMBL2218894 FLUVASTATIN SODIUM HMG-CoA reductase inhibitor 4 DailyMed

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000113161
Ensembl ENSG00000113161
GO Cellular Component GO:0005778 (peroxisomal membrane)
GO:0005783 (endoplasmic reticulum)
GO:0005789 (endoplasmic reticulum membrane)
GO:0016020 (membrane)
GO:0016021 (integral component of membrane)
GO:0043231 (intracellular membrane-bounded organelle)
GO Molecular Function GO:0004420 (hydroxymethylglutaryl-CoA reductase (NADPH) activity)
GO:0005515 (protein binding)
GO:0016491 (oxidoreductase activity)
GO:0016616 (oxidoreductase activity, acting on the CH-OH group of donors, NAD or NADP as acceptor)
GO:0042282 (hydroxymethylglutaryl-CoA reductase activity)
GO:0042803 (protein homodimerization activity)
GO:0050661 (NADP binding)
GO:0050662 (coenzyme binding)
GO:0051721 (protein phosphatase 2A binding)
GO:0070402 (NADPH binding)
GO Biological Process GO:0006629 (lipid metabolic process)
GO:0006694 (steroid biosynthetic process)
GO:0006695 (cholesterol biosynthetic process)
GO:0006743 (ubiquinone metabolic process)
GO:0007568 (aging)
GO:0007584 (response to nutrient)
GO:0008202 (steroid metabolic process)
GO:0008203 (cholesterol metabolic process)
GO:0008284 (positive regulation of cell proliferation)
GO:0008299 (isoprenoid biosynthetic process)
GO:0008542 (visual learning)
GO:0010664 (negative regulation of striated muscle cell apoptotic process)
GO:0010666 (positive regulation of cardiac muscle cell apoptotic process)
GO:0015936 (coenzyme A metabolic process)
GO:0016126 (sterol biosynthetic process)
GO:0032874 (positive regulation of stress-activated MAPK cascade)
GO:0043066 (negative regulation of apoptotic process)
GO:0043407 (negative regulation of MAP kinase activity)
GO:0045445 (myoblast differentiation)
GO:0045471 (response to ethanol)
GO:0045908 (negative regulation of vasodilation)
GO:0048643 (positive regulation of skeletal muscle tissue development)
GO:0048661 (positive regulation of smooth muscle cell proliferation)
GO:0051262 (protein tetramerization)
GO:0055114 (oxidation-reduction process)
GO:0061045 (negative regulation of wound healing)
GO:0061179 (negative regulation of insulin secretion involved in cellular response to glucose stimulus)
GO:0070374 (positive regulation of ERK1 and ERK2 cascade)
Wikipedia HMG-CoA_reductase

Target Cross References - Protein

canSAR P04035
CGD Statins, efficacy of
Human Protein Atlas ENSG00000113161
IntAct P04035
Guide to Pharmacology 639
Open Targets ENSG00000113161
PharmGKB PA189
Reactome R-HSA-191273 (Cholesterol biosynthesis.)
R-HSA-1989781 (PPARA activates gene expression.)
R-HSA-2426168 (Activation of gene expression by SREBF (SREBP).)
UniProt B7Z3Y9 P04035 Q8N190

Target Cross References - Domain

InterPro IPR000731 (SSD.)
IPR002202 (HMG_CoA_Rdtase.)
IPR004554 (HMG_CoA_Rdtase_eu_arc.)
IPR004816 (HMG_CoA_Rdtase_metazoan.)
IPR009023 (HMG_CoA_Rdtase_NAD(P)-bd_dom.)
IPR009029 (HMG_CoA_Rdtase_sub-bd_dom.)
IPR023074 (HMG_CoA_Rdtase_cat.)
IPR023076 (HMG_CoA_Rdtase_CS.)
IPR023282 (HMG_CoA_Rdtase_N.)
Pfam PF00368 (HMG-CoA_red)
PF12349 (Sterol-sensing)

Target Cross References - Structure

PDBe 1DQ8 1DQ9 1DQA 1HW8 1HW9 1HWI 1HWJ 1HWK 1HWL 2Q1L 2Q6B 2Q6C 2R4F 3BGL 3CCT 3CCW 3CCZ 3CD0 3CD5 3CD7 3CDA 3CDB
CREDO 1DQ8 1DQ9 1DQA 1HW8 1HW9 1HWI 1HWJ 1HWK 1HWL 2Q1L 2Q6B 2Q6C 2R4F 3BGL 3CCT 3CCW 3CCZ 3CD0 3CD5 3CD7 3CDA 3CDB
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