General Information of the Protein
Protein ID
PT02011
Protein Name
3-hydroxy-3-methylglutaryl-coenzyme A reductase
Gene Name
HMGCR
Sequence
MLSRLFRMHGLFVASHPWEVIVGTVTLTICMMSMNMFTGNNKICGWNYECPKFEEDVLSSDIIILTITRCIAILYIYFQFQNLRQLGSKYILGIAGLFTIFSSFVFSTVVIHFLDKELTGLNEALPFFLLLIDLSRASTLAKFALSSNSQDEVRENIARGMAILGPTFTLDALVECLVIGVGTMSGVRQLEIMCCFGCMSVLANYFVFMTFFPACVSLVLELSRESREGRPIWQLSHFARVLEEEENKPNPVTQRVKMIMSLGLVLVHAHSRWIADPSPQNSTADTSKVSLGLDENVSKRIEPSVSLWQFYLSKMISMDIEQVITLSLALLLAVKYIFFEQTETESTLSLKNPITSPVVTQKKVPDNCCRREPMLVRNNQKCDSVEEETGINRERKVEVIKPLVAETDTPNRATFVVGNSSLLDTSSVLVTQEPEIELPREPRPNEECLQILGNAEKGAKFLSDAEIIQLVNAKHIPAYKLETLMETHERGVSIRRQLLSKKLSEPSSLQYLPYRDYNYSLVMGACCENVIGYMPIPVGVAGPLCLDEKEFQVPMATTEGCLVASTNRGCRAIGLGGGASSRVLADGMTRGPVVRLPRACDSAEVKAWLETSEGFAVIKEAFDSTSRFARLQKLHTSIAGRNLYIRFQSRSGDAMGMNMISKGTEKALSKLHEYFPEMQILAVSGNYCTDKKPAAINWIEGRGKSVVCEAVIPAKVVREVLKTTTEAMIEVNINKNLVGSAMAGSIGGYNAHAANIVTAIYIACGQDAAQNVGSSNCITLMEASGPTNEDLYISCTMPSIEIGTVGGGTNLLPQQACLQMLGVQGACKDNPGENARQLARIVCGTVMAGELSLMAALAAGHLVKSHMIHNRSKINLQDLQGACTKKTA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Catalyzes the conversion of (3S)-hydroxy-3-methylglutaryl-CoA (HMG-CoA) to mevalonic acid, the rate-limiting step in the synthesis of cholesterol and other isoprenoids, thus plays a critical role in cellular cholesterol homeostasis (PubMed:2991281, PubMed:21357570, PubMed:6995544, PubMed:36745799). HMGCR is the main target of statins, a class of cholesterol-lowering drugs (PubMed:11349148, PubMed:18540668, PubMed:36745799).
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Uniprot ID
Primary ID:
P04035

Secondarily ID:
B7Z3Y9
Q8N190
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Ensembl ID
ENSG00000113161
HGNC ID
HGNC:5006
Subcellular Location
Endoplasmic reticulum membrane
Peroxisome membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000068 , A-549
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0217640
 Compound Info 
1-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-5-(4-fluorophenyl)-N,4-diphenyl-2-propan-2-ylpyrrole-3-carboxamide
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C33H36FN3O5
  2
1
IC50 = 9.2 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 5700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0217641
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate
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C25H41NO6
  2
1
IC50 = 11.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 7900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0071076
 Compound Info 
(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
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C33H35FN2O5
  1
1
IC50 = 11.6 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0252515
 Compound Info 
US9353061, Lova-HA (1)
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C24H39NO6
  1
1
IC50 = 16.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0005348
 Compound Info 
LOVASTATIN
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C24H36O5
  2
1
IC50 = 29.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 19800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0113099
 Compound Info 
US9115116, 6a
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C34H47NO5Si
  1
1
IC50 = 36.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0138667
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[4-[1-[7-(hydroxyamino)-7-oxoheptyl]triazol-4-yl]phenyl]carbamate
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C41H61N5O7Si
  2
1
IC50 = 36.5 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 22300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0159490
 Compound Info 
(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-N,3,5-trihydroxyhept-6-enamide
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C22H29FN4O6S
  2
1
IC50 = 43.7 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 14900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0064783
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[[4-[1-[7-(hydroxyamino)-7-oxoheptyl]triazol-4-yl]phenyl]methyl]carbamate
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C42H63N5O7Si
  2
1
IC50 = 53.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 16100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0116048
 Compound Info 
US9115116, 6b
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C35H49NO5Si
  1
1
IC50 = 53.8 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0108019
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[7-(hydroxyamino)-7-oxoheptyl]carbamate
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C33H56N2O7Si
  2
1
IC50 = 54.1 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 13200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0003832
 Compound Info 
N'-hydroxy-N-phenyloctanediamide
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C14H20N2O3
  1
1
IC50 > 10000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0176947
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate
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C24H39NO6
  1
1
IC50 = 15900 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000063 , Hep-G2
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0071076
 Compound Info 
(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
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C33H35FN2O5
  4
1 IC50 = 0.227 nM
2 IC50 = 6 nM
3 IC50 = 12.9 nM
4 Ki = 6.2 nM
CP0005348
 Compound Info 
LOVASTATIN
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C24H36O5
  6
1 IC50 = 2 nM
2 IC50 = 2.2 nM
3 IC50 = 20 nM
4 IC50 = 29.5 nM
5 IC50 = 20100 nM
6 Ki = 0.6 nM
CP0217640
 Compound Info 
1-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-5-(4-fluorophenyl)-N,4-diphenyl-2-propan-2-ylpyrrole-3-carboxamide
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C33H36FN3O5
  1
1 IC50 = 12.3 nM
CP0217641
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] 2,2-dimethylbutanoate
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C25H41NO6
  1
1 IC50 = 13.1 nM
CP0176947
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[(3R,5R)-3,5-dihydroxy-7-(hydroxyamino)-7-oxoheptyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] (2S)-2-methylbutanoate
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C24H39NO6
  1
1 IC50 = 16.8 nM
CP0138667
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[4-[1-[7-(hydroxyamino)-7-oxoheptyl]triazol-4-yl]phenyl]carbamate
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C41H61N5O7Si
  1
1 IC50 = 36.5 nM
CP0159490
 Compound Info 
(E,3R,5S)-7-[4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-propan-2-ylpyrimidin-5-yl]-N,3,5-trihydroxyhept-6-enamide
   Show/Hide
C22H29FN4O6S
  1
1 IC50 = 43.7 nM
CP0064783
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[[4-[1-[7-(hydroxyamino)-7-oxoheptyl]triazol-4-yl]phenyl]methyl]carbamate
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C42H63N5O7Si
  1
1 IC50 = 53.8 nM
CP0108019
 Compound Info 
[(1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-[tert-butyl(dimethyl)silyl]oxy-6-oxooxan-2-yl]ethyl]-3,7-dimethyl-1,2,3,7,8,8a-hexahydronaphthalen-1-yl] N-[7-(hydroxyamino)-7-oxoheptyl]carbamate
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C33H56N2O7Si
  1
1 IC50 = 54.1 nM
CP0735346
 Compound Info 
Sodium salt 9,9-bis-(4-fluoro-phenyl)-3,5-dihydroxy-8-(1-methyl-1H-tetrazol-5-yl)-nona-6,8-dienoate
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C23H21F2N4NaO4
  1
1 IC50 = 3000 nM
CP0003832
 Compound Info 
N'-hydroxy-N-phenyloctanediamide
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C14H20N2O3
  1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( HMG-CoA reductase (HMGCR) )
Target Type Successful Target
Disease 7 Target-related Diseases  7
1 Pain [ICD-11: MG30-MG3Z]
2 Cardiovascular disease [ICD-11: BA00-BE2Z]
3 Hyperlipidaemia [ICD-11: 5C80]
4 Hypercholesterolaemia [ICD-11: 5C80.0]
5 Dyslipidemia [ICD-11: 5C80-5C81]
6 Coronary heart disease [ICD-11: BA80.Z]
7 Arteriosclerosis [ICD-11: BD40]
Approved Drug(s) 12 Approved Drugs  12
1 Aspirin
 Drug Info 
Approved
Pain
2 Atorvastatin
 Drug Info 
Approved
Cardiovascular disease
3 Cerivastatin
 Drug Info 
Approved
Hyperlipidaemia
4 Fluvastatin
 Drug Info 
Approved
Hypercholesterolaemia
5 Lovastatin
 Drug Info 
Approved
Hypercholesterolaemia
6 PITAVASTATIN CALCIUM
 Drug Info 
Approved
Dyslipidemia
7 Pravastatin
 Drug Info 
Approved
Hypercholesterolaemia
8 Rosuvastatin
 Drug Info 
Approved
Hypercholesterolaemia
9 Simvastatin
 Drug Info 
Approved
Hypercholesterolaemia
10 Teriflunomide
 Drug Info 
Approved
Hyperlipidaemia
11 TOCOTRIENOL
 Drug Info 
Approved
Hyperlipidaemia
12 LAROPIPRANT
 Drug Info 
Phase 4
Coronary heart disease
Discontinued Drug(s) 3 Discontinued Drugs  3
1 GLENVASTATIN
 Drug Info 
Discontinued in Phase 2
Hyperlipidaemia
2 BMY-22089
 Drug Info 
Terminated
Hyperlipidaemia
3 SR12813
 Drug Info 
Terminated
Arteriosclerosis
Investigative Drug(s) 1 Investigative Drug  1
1 Statin
 Drug Info 
Investigative
Hypercholesterolaemia
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT07548 3-hydroxy-3-methylglutaryl-coenzyme A reductase Cricetulus griseus, Chinese hamster, Cricetulus barabensis griseus
 Protein Info