1.1.1.34: hydroxymethylglutaryl-CoA reductase (NADPH)

This is an abbreviated version, for detailed information about hydroxymethylglutaryl-CoA reductase (NADPH), go to the full flat file.

Reaction

(R)-mevalonate
+
CoA
+ 2 NADP+ =
(S)-3-hydroxy-3-methylglutaryl-CoA
+ 2 NADPH + 2 H+

Synonyms

3-hydroxy-3-methyl-glutaryl CoA reductase, 3-hydroxy-3-methylglutaryl Ccoenzyme A reductase 1, 3-hydroxy-3-methylglutaryl co-enzyme A reductase, 3-hydroxy-3-methylglutaryl CoA reductase, 3-hydroxy-3-methylglutaryl coenzyme A reductase, 3-hydroxy-3-methylglutaryl coenzyme A reductase 1, 3-hydroxy-3-methylglutaryl-CoA reductase, 3-hydroxy-3-methylglutaryl-CoA reductase (NADPH), 3-hydroxy-3-methylglutaryl-coenzyme A reductase, 3-hydroxymethylglutaryl coenzyme A reductase, acetoacetyl-coenzyme A thiolase/3-hydroxy-3-methylglutaryl-coenzyme A reductase, beta-hydroxy-beta-methylglutaryl coenzyme A reductase, beta-hydroxy-beta-methylglutaryl-Co A reductase, EuHMGR, HMG CoA reductase, HMG-CoA reductase, HMG-CoAR, HMG1, HMG2, HMG2.2, Hmg2p, HMG3.3, HMGCoA reductase, HMGCoA reductase-mevalonate:NADP-oxidoreductase (acetylating CoA), HMGCoAR, HMGCR, HMGR, HMGR1, HMGR1S, HMGR2, hydroxy-3-methylglutoryl-Coenzyme A reductase, hydroxymethylglutaryl CoA reductase (NADPH), hydroxymethylglutaryl-coenzyme A reductase (reduced nicotinamide adenine dinucleotide phosphate), mevalonate:NADP+ oxidoreductase (acetylating CoA), microsomal HMG-CoA reductase, NADPH-hydroxymethylglutaryl-CoA reductase, S-3-hydroxy-3-methylglutaryl-CoA reductase

ECTree

     1 Oxidoreductases
         1.1 Acting on the CH-OH group of donors
             1.1.1 With NAD+ or NADP+ as acceptor
                1.1.1.34 hydroxymethylglutaryl-CoA reductase (NADPH)

IC50 Value

IC50 Value on EC 1.1.1.34 - hydroxymethylglutaryl-CoA reductase (NADPH)

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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00000035
(3R,5R)-7-(1-ethyl-3-(4-fluorophenyl)-4-methyl-5-[(5-methyl-pyrazin-2-ylmethyl)-carbamoyl]-1H-pyrrol-2-yl)-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000029
(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-4-methyl-5-phenylcarbamoyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000024
(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-5-(4-methoxybenzylcarbamoyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000028
(3R,5R)-7-[1-ethyl-3-(4-fluorophenyl)-5-(4-methoxycarbonyl-benzylcarbamoyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000017
(3R,5R)-7-[3-(4-fluoro-phenyl)-1-isopropyl-5-phenylcarbamoyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000043
(3R,5R)-7-[3-(4-fluorophenyl)-1-isopropyl-4-phenyl-5-phenylcarbamoyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.0000018
(3R,5R)-7-[3-(4-fluorophenyl)-5-[(3-methoxybenzyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000007
(3R,5R)-7-[3-(4-fluorophenyl)-5-[[4-(methoxymethyl)benzyl]carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.00000011
(3R,5R)-7-[5-(4-carboxy-benzylcarbamoyl)-ethyl-3-(4-fluorophenyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid disodium salt
Rattus norvegicus
-
37C, hepatocytes
0.00000015
(3R,5R)-7-[5-benzylcarbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid
Rattus norvegicus
-
37C, hepatocytes
0.000032
(3R,5R)-7-[5-carbamoyl-1-ethyl-3-(4-fluorophenyl)-4-methyl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoic acid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.0000049
(3R,5R)-7-[5-carbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoicacid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.0000021
(3R,5R)-7-[5-cyano-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.0000012
(3R,5R)-7-[5-[(3-carbamoylbenzyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000002
(3R,5R)-7-[5-[(4-cyanobenzyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000012
(3R,5R)-7-[5-[[4-(dimethylcarbamoyl)benzyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
2.2 - 26
(E,3R,5S)-7-(4-(3-(4-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoic acid
0.0000022
4-[[([5-[(3R,5R)-6-carboxy-3,5-dihydroxyhexyl]-4-(4-fluorophenyl)-1-(1-methylethyl)-3-phenyl-1H-pyrrol-2-yl]carbonyl)amino]methyl]benzoic acid
Mus musculus
-
inhibition of purified enzyme
0.0000018
7-[3,4-bis(4-fluorophenyl)-1-(1-methylethyl)-5-(phenylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000007
7-[3,4-bis(4-fluorophenyl)-5-[(3-hydroxyphenyl)carbamoyl]-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000066
7-[3,4-bis(4-fluorophenyl)-5-[(3-methoxyphenyl)carbamoyl]-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000124
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-(phenylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.000015
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-(propylcarbamoyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000029
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-[(4-sulfamoylphenyl)carbamoyl]-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000008
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-5-[(pyridin-2-ylmethyl)carbamoyl]-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000015
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000034
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(5-methyl-1H-imidazol-2-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000026
7-[3-(4-fluorophenyl)-1-(1-methylethyl)-5-[[(5-methyl-1H-pyrazol-3-yl)methyl]carbamoyl]-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000088
7-[3-(4-fluorophenyl)-5-(methylcarbamoyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000004
7-[3-(4-fluorophenyl)-5-[(4-hydroxyphenyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000008
7-[3-(4-fluorophenyl)-5-[(4-methoxybenzyl)carbamoyl]-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000008
7-[5-(benzylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000038
7-[5-(cyclopropylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.00002
7-[5-(dimethylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.000012
7-[5-(ethylcarbamoyl)-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.000003
7-[5-carbamoyl-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000051
7-[5-ethylcarbamoyl-3-(4-fluoro-phenyl)-1-isopropyl-4-pyridin-2-yl-1H-pyrrol-2-yl]-3,5-dihydroxy-heptanoicacid sodium salt
Rattus norvegicus
-
37C, hepatocytes
0.0000003
7-[5-[(4-carbamoylphenyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000003
7-[5-[(4-carboxyphenyl)carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000006
7-[5-[[(1,5-dimethyl-1H-pyrazol-3-yl)methyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000003
7-[5-[[3-(dimethylcarbamoyl)phenyl]carbamoyl]-3,4-bis(4-fluorophenyl)-1-(1-methylethyl)-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
0.0000014
7-[5-[[4-(dimethylcarbamoyl)phenyl]carbamoyl]-3-(4-fluorophenyl)-1-(1-methylethyl)-4-phenyl-1H-pyrrol-2-yl]-3,5-dihydroxyheptanoate
Mus musculus
-
inhibition of purified enzyme
1.2
8-hydroxygeraniol
Phaedon cochleariae
-
pH 6.8, 30C, recombinant catalytic domain
0.00049
AFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0000017
cerivastatin
Rattus norvegicus
-
37C, hepatocytes
0.00016
DFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.00024
EFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0038
F(4-fluoro)VAE
Rattus norvegicus
-
-
0.00032
FFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0025
FFYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0085
FG-(4-fluoro)FVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0004
FGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.00022 - 0.003
fluvastatin
0.0014
FPYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0438
FVAE
Rattus norvegicus
-
-
0.00027
GFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0015
GFPDGG
Rattus norvegicus
-
-
0.0017
GFPEGG
Rattus norvegicus
-
-
0.0169
GFPTGG
Rattus norvegicus
-
-
0.0223
GLPDGG
Rattus norvegicus
-
-
0.0272
GLPEGG
Rattus norvegicus
-
-
0.0194
GLPTGG
Rattus norvegicus
-
-
0.0752
IAVE
Rattus norvegicus
-
-
0.097
IAVP
Rattus norvegicus
-
-
0.152
IAVPGEVA
Rattus norvegicus
-
-
0.152
IAVPTGVA
Homo sapiens
-
pH and temperature not specified in the publication
0.00035
IFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.075
Ile-Ala-Val-Glu
Homo sapiens
-
pH and temperature not specified in the publication
0.201
Ile-Ala-Val-Pro-Gly-Glu-Val-Ala
Homo sapiens
-
pH and temperature not specified in the publication
0.052
Ile-Val-Ala-Glu
Homo sapiens
-
pH and temperature not specified in the publication
0.0441
IVAE
Rattus norvegicus
-
-
0.484
Leu-Pro-Tyr-Pro
Homo sapiens
-
pH and temperature not specified in the publication
0.00037
LFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.484
LPYP
Rattus norvegicus
-
-
0.04
mevastatin
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
0.00043
PFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.00000023 - 0.0000031
rosuvastatin
0.000033
SFGYVAE peptide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000013 - 0.000049
simvastatin
0.82
sodium (E,3R,5S)-7-(2-(2-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
1.2
sodium (E,3R,5S)-7-(2-(3-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
0.15
sodium (E,3R,5S)-7-(2-(4-fluorophenyl)-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxy-hept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
0.85
sodium (E,3R,5S)-7-(2-phenyl-4-(3-phenylpentan-3-yl)phenyl)-3,5-dihydroxyhept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
7.4
sodium (E,3R,5S)-7-(4-(3-(2-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
92
sodium (E,3R,5S)-7-(4-(3-(3-fluorophenyl)pentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (3.7 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
1.8
sodium (E,3R,5S)-7-(4-(3-phenylpentan-3-yl)-2-isopropylphenyl)-3,5-dihydroxyhept-6-enoate
Rattus norvegicus
-
DL-[3-14C]3-hydroxy-3-methylglutaryl-CoA (0.37 MBq) and 10 mg protein of microsomal fraction incubated at 37C for 30 min
0.00026
TFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.044
Tyr-Ala-Val-Glu
Homo sapiens
-
pH and temperature not specified in the publication
0.041
Tyr-Val-Ala-Glu
Homo sapiens
-
pH and temperature not specified in the publication
0.00045
VFGYVAE
Homo sapiens
-
pH and temperature not specified in the publication
0.0526
YAVE
Rattus norvegicus
-
-
0.0418
YVAE
Rattus norvegicus
-
-