General Information of the Protein
Protein ID
PT05526
Protein Name
Phospholipid hydroperoxide glutathione peroxidase GPX4
Secondarily
Protein Name
Glutathione peroxidase 4
Gene Name
GPX4
Sequence
MSLGRLCRLLKPALLCGALAAPGLAGTMCASRDDWRCARSMHEFSAKDIDGHMVNLDKYRGFVCIVTNVASQUGKTEVNYTQLVDLHARYAECGLRILAFPCNQFGKQEPGSNEEIKEFAAGYNVKFDMFSKICVNGDDAHPLWKWMKIQPKGKGILGNAIKWNFTKFLIDKNGCVVKRYGPMEEPLVIEKDLPHYF
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Essential antioxidant peroxidase that directly reduces phospholipid hydroperoxide even if they are incorporated in membranes and lipoproteins (By similarity). Can also reduce cholesterol hydroperoxide and thymine hydroperoxide (By similarity). Plays a key role in protecting cells from oxidative damage by preventing membrane lipid peroxidation (By similarity). Required to prevent cells from ferroptosis, a non-apoptotic cell death resulting from an iron-dependent accumulation of lipid reactive oxygen species (PubMed:24439385). The presence of selenocysteine (Sec) versus Cys at the active site is essential for life: it provides resistance to overoxidation and prevents cells against ferroptosis (By similarity). The presence of Sec at the active site is also essential for the survival of a specific type of parvalbumin-positive interneurons, thereby preventing against fatal epileptic seizures (By similarity). May be required to protect cells from the toxicity of ingested lipid hydroperoxides (By similarity). Required for normal sperm development and male fertility (By similarity). Essential for maturation and survival of photoreceptor cells (By similarity). Plays a role in a primary T-cell response to viral and parasitic infection by protecting T-cells from ferroptosis and by supporting T-cell expansion (By similarity). Plays a role of glutathione peroxidase in platelets in the arachidonic acid metabolism (PubMed:11115402). Reduces hydroperoxy ester lipids formed by a 15-lipoxygenase that may play a role as down-regulator of the cellular 15-lipoxygenase pathway (By similarity). Can reduce fatty acid-derived hydroperoxides (PubMed:11115402, PubMed:36608588). Can also reduce small soluble hydroperoxides such as H2O2, cumene hydroperoxide and tert-butyl hydroperoxide (PubMed:36608588, PubMed:17630701).
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Uniprot ID
Primary ID:
P36969

Secondarily ID:
O43381
Q6PJ59
Q9UPK2
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Ensembl ID
ENSG00000167468
HGNC ID
HGNC:4556
Subcellular Location
Mitochondrion
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: CL000561 , LOX-IMVI
Compound ID Compound Name Compound Formula
CP0917680
(1S,3R)-methyl 2-(2-chloroacetyl)-1-(4-(methoxycarbonyl)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate
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C23H21ClN2O5
 2
1
EC50 = 12 nM
   TI
   LI
   LO
   TS
2
EC50 = 3800 nM
   TI
   LI
   LO
   TS
CP0133489
2-(3-chloro-N-(2-chloro-1-oxoethyl)-4-methoxyanilino)-N-(2-phenylethyl)-2-thiophen-2-ylacetamide
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C23H22Cl2N2O3S
 2
1
EC50 = 28 nM
   TI
   LI
   LO
   TS
2
EC50 = 2200 nM
   TI
   LI
   LO
   TS
CP0479526
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(5-methyl-4-nitro-1,2-oxazol-3-yl)methanone
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C22H20Cl2N4O4
 2
1
EC50 = 44 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479507
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]prop-2-ynamide
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C24H21ClN2O3S
 2
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
2
EC50 = 19800 nM
   TI
   LI
   LO
   TS
CP0491514
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]-3-trimethylsilylprop-2-ynamide
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C27H29ClN2O3SSi
 2
1
EC50 = 210 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0468757
2-chloro-N-heptyl-N-(3-methylphenyl)acetamide
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C16H24ClNO
 2
1
EC50 = 340 nM
   TI
   LI
   LO
   TS
2
EC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0479522
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]-3-triethylsilylprop-2-ynamide
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C30H35ClN2O3SSi
 2
1
EC50 = 370 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479509
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-2-chloroethanone
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C19H19Cl3N2O
 2
1
EC50 = 420 nM
   TI
   LI
   LO
   TS
2
EC50 = 4200 nM
   TI
   LI
   LO
   TS
CP0500339
2-(N-(2-bromoacetyl)-3-chloro-4-methoxyanilino)-N-(2-phenylethyl)-2-thiophen-2-ylacetamide
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C23H22BrClN2O3S
 2
1
EC50 = 600 nM
   TI
   LI
   LO
   TS
2
EC50 = 5200 nM
   TI
   LI
   LO
   TS
CP0500348
N-(3-chloro-4-methoxyphenyl)-3-[dimethyl(phenyl)silyl]-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]prop-2-ynamide
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C32H31ClN2O3SSi
 2
1
EC50 = 1000 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479523
2-chloro-1-(1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl)ethanone
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C13H13ClN2O
 2
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
2
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0515096
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]prop-2-yn-1-one
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C20H18Cl2N2O
 2
1
EC50 = 1200 nM
   TI
   LI
   LO
   TS
2
EC50 = 3600 nM
   TI
   LI
   LO
   TS
CP0439662
MLS001172197
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C19H18ClNO4
 2
1
EC50 = 1600 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500342
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-3-trimethylsilylprop-2-yn-1-one
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C23H26Cl2N2OSi
 2
1
EC50 = 1800 nM
   TI
   LI
   LO
   TS
2
EC50 = 4800 nM
   TI
   LI
   LO
   TS
CP0513512
N-heptyl-5-methyl-N-(3-methylphenyl)-4-nitro-1,2-oxazole-3-carboxamide
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C19H25N3O4
 2
1
EC50 = 5800 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0571774
(3Z)-N-(3-chloro-4-methoxyphenyl)-3-hydroxyimino-3-nitro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]propanamide
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C24H23ClN4O6S
 2
1
EC50 = 10100 nM
   TI
   LI
   LO
   TS
2
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479510
methyl (E)-4-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-4-oxobut-2-enoate
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C22H22Cl2N2O3
 2
1
EC50 = 18000 nM
   TI
   LI
   LO
   TS
2
EC50 = 19000 nM
   TI
   LI
   LO
   TS
CP0548279
(E)-2-[4-[bis(4-chlorophenyl)methyl]piperazine-1-carbonyl]but-2-enenitrile
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C22H21Cl2N3O
 2
1
EC50 = 22000 nM
   TI
   LI
   LO
   TS
2
EC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0565180
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]but-2-yn-1-one
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C21H20Cl2N2O
 2
1
EC50 = 24000 nM
   TI
   LI
   LO
   TS
2
EC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0500347
(E)-1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-3-nitroprop-2-en-1-one
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C20H19Cl2N3O3
 2
1
EC50 = 30000 nM
   TI
   LI
   LO
   TS
2
EC50 = 31000 nM
   TI
   LI
   LO
   TS
CP0515093
N-(3-chloro-4-methoxyphenyl)-4-hydroxy-4-methyl-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]pent-2-ynamide
   Show/Hide
C27H27ClN2O4S
 2
1
EC50 = 32000 nM
   TI
   LI
   LO
   TS
2
EC50 = 33000 nM
   TI
   LI
   LO
   TS
CP0479524
N-(3-chloro-4-methoxyphenyl)-5-methyl-4-nitro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]-1,2-oxazole-3-carboxamide
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C26H23ClN4O6S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479525
N-(3-chloro-4-methoxyphenyl)-3-nitro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]propanamide
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C24H24ClN3O5S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500344
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]prop-2-enamide
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C24H23ClN2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500345
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]prop-2-en-1-one
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C20H20Cl2N2O
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500346
(E)-1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]but-2-en-1-one
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C21H22Cl2N2O
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0512775
2-bromo-N-(3-chloro-4-methoxyphenyl)-2,2-difluoro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]acetamide
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C23H20BrClF2N2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0512776
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(2-chloropyridin-4-yl)methanone
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C23H20Cl3N3O
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0513513
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]propane-1,2-dione
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C20H20Cl2N2O2
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0545888
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]but-2-ynamide
   Show/Hide
C25H23ClN2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0552335
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(2-chloropyridin-3-yl)methanone
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C23H20Cl3N3O
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0565545
2-chloro-N-(3-chloro-4-methoxyphenyl)-2,2-difluoro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]acetamide
   Show/Hide
C23H20Cl2F2N2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0568517
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(2,5-difluoro-4-nitrophenyl)methanone
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C24H19Cl2F2N3O3
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0955514
(1R,3R)-methyl 1-(4-(methoxycarbonyl)phenyl)-2-(5-methyl-4-nitroisoxazole-3-carbonyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate
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C26H22N4O8
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0957136
(1R,3R)-methyl 2-(2-chloroacetyl)-1-(4-(methoxycarbonyl)phenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate
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C23H21ClN2O5
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479518
2-(N-(2-bromo-2-fluoroacetyl)-3-chloro-4-methoxyanilino)-N-(2-phenylethyl)-2-thiophen-2-ylacetamide
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C23H21BrClFN2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479519
N-(3-chloro-4-methoxyphenyl)-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]-3-tri(propan-2-yl)silylprop-2-ynamide
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C33H41ClN2O3SSi
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0479520
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(2-chloro-3-nitrophenyl)methanone
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C24H20Cl3N3O3
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500341
2-chloro-N-(3-chloro-4-methoxyphenyl)-2,3,3,3-tetrafluoro-N-[2-oxo-2-(2-phenylethylamino)-1-thiophen-2-ylethyl]propanamide
   Show/Hide
C24H20Cl2F4N2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0500343
1-[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-2-(3-bromo-4,5-dihydro-1,2-oxazol-5-yl)ethanone
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C22H22BrCl2N3O2
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0512774
N-(1,3-benzodioxol-5-yl)-5-methyl-4-nitro-N-[(2-prop-2-enoxyphenyl)methyl]-1,2-oxazole-3-carboxamide
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C22H19N3O7
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0540504
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(3-bromo-4,5-dihydro-1,2-oxazol-5-yl)methanone
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C21H20BrCl2N3O2
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0548274
2-(3-chloro-N-(2-chloro-2-fluoroacetyl)-4-methoxyanilino)-N-(2-phenylethyl)-2-thiophen-2-ylacetamide
   Show/Hide
C23H21Cl2FN2O3S
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0565544
[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]-(2-fluoro-5-nitrophenyl)methanone
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C24H20Cl2FN3O3
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0571773
(5-methyl-4-nitro-1,2-oxazol-3-yl)-(1,3,4,9-tetrahydropyrido[3,4-b]indol-2-yl)methanone
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C16H14N4O4
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0952577
(1S,3R)-methyl 1-(4-(methoxycarbonyl)phenyl)-2-(5-methyl-4-nitroisoxazole-3-carbonyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxylate
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C26H22N4O8
 1
1
EC50 > 33000 nM
   TI
   LI
   LO
   TS
CP0266261
5-methyl-4-nitro-N-prop-2-ynyl-1,2-oxazole-3-carboxamide
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C8H7N3O4
 1
1
EC50 = 48000 nM
   TI
   LI
   LO
   TS