General Information of the Protein
Protein ID
PT00940
Protein Name
Prostaglandin G/H synthase 1
Secondarily
Protein Name
Cyclooxygenase-1
Prostaglandin H2 synthase 1
Prostaglandin-endoperoxide synthase 1
Gene Name
PTGS1
Secondarily
Gene Name
COX1
Sequence
MSRSLLLWFLLFLLLLPPLPVLLADPGAPTPVNPCCYYPCQHQGICVRFGLDRYQCDCTRTGYSGPNCTIPGLWTWLRNSLRPSPSFTHFLLTHGRWFWEFVNATFIREMLMRLVLTVRSNLIPSPPTYNSAHDYISWESFSNVSYYTRILPSVPKDCPTPMGTKGKKQLPDAQLLARRFLLRRKFIPDPQGTNLMFAFFAQHFTHQFFKTSGKMGPGFTKALGHGVDLGHIYGDNLERQYQLRLFKDGKLKYQVLDGEMYPPSVEEAPVLMHYPRGIPPQSQMAVGQEVFGLLPGLMLYATLWLREHNRVCDLLKAEHPTWGDEQLFQTTRLILIGETIKIVIEEYVQQLSGYFLQLKFDPELLFGVQFQYRNRIAMEFNHLYHWHPLMPDSFKVGSQEYSYEQFLFNTSMLVDYGVEALVDAFSRQIAGRIGGGRNMDHHILHVAVDVIRESREMRLQPFNEYRKRFGMKPYTSFQELVGEKEMAAELEELYGDIDALEFYPGLLLEKCHPNSIFGESMIEIGAPFSLKGLLGNPICSPEYWKPSTFGGEVGFNIVKTATLKKLVCLNTKTCPYVSFRVPDASQDDGPAVERPSTEL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Dual cyclooxygenase and peroxidase that plays an important role in the biosynthesis pathway of prostanoids, a class of C20 oxylipins mainly derived from arachidonate ((5Z,8Z,11Z,14Z)-eicosatetraenoate, AA, C20:4(n-6)), with a particular role in the inflammatory response. The cyclooxygenase activity oxygenates AA to the hydroperoxy endoperoxide prostaglandin G2 (PGG2), and the peroxidase activity reduces PGG2 to the hydroxy endoperoxide prostaglandin H2 (PGH2), the precursor of all 2-series prostaglandins and thromboxanes. This complex transformation is initiated by abstraction of hydrogen at carbon 13 (with S-stereochemistry), followed by insertion of molecular O2 to form the endoperoxide bridge between carbon 9 and 11 that defines prostaglandins. The insertion of a second molecule of O2 (bis-oxygenase activity) yields a hydroperoxy group in PGG2 that is then reduced to PGH2 by two electrons (PubMed:7947975). Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the generation of thromboxane A2 (TXA2), which promotes platelet activation and aggregation, vasoconstriction and proliferation of vascular smooth muscle cells (Probable). Can also use linoleate (LA, (9Z,12Z)-octadecadienoate, C18:2(n-6)) as substrate and produce hydroxyoctadecadienoates (HODEs) in a regio- and stereospecific manner, being (9R)-HODE ((9R)-hydroxy-(10E,12Z)-octadecadienoate) and (13S)-HODE ((13S)-hydroxy-(9Z,11E)-octadecadienoate) its major products (By similarity).
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Uniprot ID
Primary ID:
P23219

Secondarily ID:
A8K1V7
B4DHQ2
B4E2S5
Q15122
Q3HY28
Q3HY29
Q5T7T6
Q5T7T7
Q5T7T8
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Ensembl ID
ENSG00000095303
HGNC ID
HGNC:9604
Subcellular Location
Microsome membrane
Endoplasmic reticulum 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: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0010057
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
   Show/Hide
C19H16ClNO4
 2
1
IC50 = 18 nM
   TI
   LI
   LO
   TS
2
IC50 = 39 nM
   TI
   LI
   LO
   TS
CP0511926
3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-1-(4-methoxyphenyl)-5-phenyl-1H-pyrazole
   Show/Hide
C29H29FN2O4
 1
1
IC50 = 36 nM
   TI
   LI
   LO
   TS
CP0061060
5-Bromo-2-(4-fluoro-phenyl)-3-(4-methanesulfonyl-phenyl)-thiophene
   Show/Hide
C17H12BrFO2S2
 1
1
IC50 = 59 nM
   TI
   LI
   LO
   TS
CP0448740
6-(4-Methylsulfanyl-phenyl)-5-phenyl-imidazo[2,1-b]thiazole
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C18H14N2S2
 1
1
IC50 = 78 nM
   TI
   LI
   LO
   TS
CP0460409
1-(4,4-Dimethyl-3-methylene-2-phenyl-cyclobut-1-enyl)-4-methanesulfonyl-benzene
   Show/Hide
C20H20O2S
 1
1
IC50 = 120 nM
   TI
   LI
   LO
   TS
CP0049684
5-(4-Fluoro-phenyl)-6-(4-methanesulfonyl-phenyl)-spiro[2.4]hept-5-ene
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C20H19FO2S
 1
1
IC50 = 140 nM
   TI
   LI
   LO
   TS
CP0404461
5-(4-Methylsulfanyl-phenyl)-6-phenyl-imidazo[2,1-b]thiazole
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C18H14N2S2
 1
1
IC50 = 320 nM
   TI
   LI
   LO
   TS
CP0377648
2-(4-Fluoro-phenyl)-3-(4-methanesulfonyl-phenyl)-4,4-dimethyl-cyclobut-2-enone
   Show/Hide
C19H17FO3S
 1
1
IC50 = 370 nM
   TI
   LI
   LO
   TS
CP0395145
3-(4-Methanesulfonyl-phenyl)-2-phenyl-spiro[3.4]oct-2-en-1-one
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C21H20O3S
 1
1
IC50 = 500 nM
   TI
   LI
   LO
   TS
CP0470554
1-Methanesulfonyl-4-(3-methylene-2-phenyl-cyclobut-1-enyl)-benzene
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C18H16O2S
 1
1
IC50 = 540 nM
   TI
   LI
   LO
   TS
CP0428132
2-Isopropyl-5-(4-methanesulfonyl-phenyl)-6-phenyl-thiazolo[3,2-b][1,2,4]triazole
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C20H19N3O2S2
 1
1
IC50 = 600 nM
   TI
   LI
   LO
   TS
CP0449755
5-(4-Methanesulfonyl-phenyl)-6-m-tolyl-2-trifluoromethyl-thiazolo[3,2-b][1,2,4]triazole
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C19H14F3N3O2S2
 1
1
IC50 = 610 nM
   TI
   LI
   LO
   TS
CP0401298
5-(4-Methanesulfonyl-phenyl)-6-phenyl-2-trifluoromethyl-thiazolo[3,2-b][1,2,4]triazole
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C18H12F3N3O2S2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0405545
3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-1-(4-fluorophenyl)-5-phenyl-1H-pyrazole
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C28H26F2N2O3
 1
1
IC50 = 1130 nM
   TI
   LI
   LO
   TS
CP0475206
3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-1-(4-methylphenyl)-5-phenyl-1H-pyrazole
   Show/Hide
C29H29FN2O3
 1
1
IC50 = 1560 nM
   TI
   LI
   LO
   TS
CP0405546
1-(4-chlorophenyl)-3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C28H26ClFN2O3
 1
1
IC50 = 1810 nM
   TI
   LI
   LO
   TS
CP0383216
2-(4-Methanesulfonyl-phenyl)-4,4-dimethyl-3-phenyl-cyclobut-2-enone
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C19H18O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0475726
3-(4-Methanesulfonyl-phenyl)-4,4-dimethyl-2-phenyl-cyclobut-2-enone
   Show/Hide
C19H18O3S
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0441647
5-(4-Methanesulfonyl-phenyl)-6-phenyl-thiazolo[2,3-c][1,2,4]triazole
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C17H13N3O2S2
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0449758
2-Ethyl-5-(4-methanesulfonyl-phenyl)-6-phenyl-thiazolo[3,2-b][1,2,4]triazole
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C19H17N3O2S2
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0489046
3-(4-Methanesulfonyl-phenyl)-2-phenyl-cyclobut-2-enone
   Show/Hide
C17H14O3S
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0420498
3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-1,5-diphenyl-1H-pyrazole
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C28H27FN2O3
 1
1
IC50 = 7140 nM
   TI
   LI
   LO
   TS
CP0498180
6-(3-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-2-trifluoromethyl-thiazolo[3,2-b][1,2,4]triazole
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C18H11F4N3O2S2
 1
1
IC50 = 8500 nM
   TI
   LI
   LO
   TS
CP0405020
6-(4-Methanesulfonyl-phenyl)-5-phenyl-2-trifluoromethyl-thiazolo[3,2-b][1,2,4]triazole
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C18H12F3N3O2S2
 1
1
IC50 = 9000 nM
   TI
   LI
   LO
   TS
CP0430344
5-(4-Methanesulfonyl-phenyl)-6-phenyl-2-vinyl-thiazolo[3,2-b][1,2,4]triazole
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C19H15N3O2S2
 1
1
IC50 = 9600 nM
   TI
   LI
   LO
   TS
CP0011191
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene-1-sulfonamide
   Show/Hide
C17H14F3N3O2S
 1
1
IC50 = 13500 nM
   TI
   LI
   LO
   TS
CP0502197
6-(4-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C17H12FN3O2S2
 1
1
IC50 = 15000 nM
   TI
   LI
   LO
   TS
CP0427141
1-(4-methanesulfonylphenyl)-3-[(3,4-methylenedioxy)-phenoxymethyl]-5-phenyl-1H-pyrazole
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C24H20N2O5S
 1
1
IC50 = 15810 nM
   TI
   LI
   LO
   TS
CP0437319
1-(4-methanesulfonylphenyl)-3-[(3,4,5-trimethoxy)phenoxymethyl]-5-phenyl-1H-pyrazole
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C26H26N2O6S
 1
1
IC50 = 17590 nM
   TI
   LI
   LO
   TS
CP0522693
1-(4-methanesulfonylphenyl)-3-[(3,5-dimethoxy)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C25H24N2O5S
 1
1
IC50 = 25050 nM
   TI
   LI
   LO
   TS
CP0420193
1-(4-aminosulfonylphenyl)-3-[3-fluoro-5-(4-methoxytetrahydropyran-4-yl)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C28H28FN3O5S
 1
1
IC50 = 25700 nM
   TI
   LI
   LO
   TS
CP0096361
3-((3-fluoro-5-(1-methoxycyclohexyl)phenoxy)methyl)-1-(4-(methylsulfonyl)phenyl)-5-phenyl-1H-pyrazole
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C29H29FN2O5S
 1
1
IC50 = 26080 nM
   TI
   LI
   LO
   TS
CP0437782
6-(3,4-Difluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-thiazolo[3,2-b][1,2,4]triazole
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C17H11F2N3O2S2
 1
1
IC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0879971
3-(4-Methanesulfonyl-phenyl)-4,4-dimethyl-2-phenyl-cyclobut-2-enone oxime
   Show/Hide
C19H19NO3S
 1
1
IC50 = 34000 nM
   TI
   LI
   LO
   TS
CP0427142
1-(4-methanesulfonylphenyl)-3-[3-(4-morpholino)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C27H27N3O4S
 1
1
IC50 = 38080 nM
   TI
   LI
   LO
   TS
CP0498156
5-(4-Methanesulfonyl-phenyl)-6-phenyl-thiazolo[3,2-b][1,2,4]triazole
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C17H13N3O2S2
 1
1
IC50 = 43000 nM
   TI
   LI
   LO
   TS
CP0427145
3-[(3-fluoro-5-methoxy)phenoxymethyl]-1-(4-methanesulfonylphenyl)-5-phenyl-1H-pyrazole
   Show/Hide
C24H21FN2O4S
 1
1
IC50 = 44330 nM
   TI
   LI
   LO
   TS
CP0535156
3-(4-Methanesulfonyl-phenyl)-4,4-dimethyl-2-phenyl-cyclobut-2-enol
   Show/Hide
C19H20O3S
 1
1
IC50 = 45000 nM
   TI
   LI
   LO
   TS
CP0376557
6-(4-Methanesulfonyl-phenyl)-2,3-dimethyl-5-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C20H18N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0383382
2-Chloro-6-(4-chloro-phenyl)-5-(4-methanesulfonyl-phenyl)-imidazo[2,1-b]thiazole
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C18H12Cl2N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0402232
5-(4-Methanesulfonyl-phenyl)-6-phenyl-imidazo[2,1-b]thiazole-3-carboxylic acid
   Show/Hide
C19H14N2O4S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0402569
5-(4-Methanesulfonyl-phenyl)-6-phenyl-3,5-dihydro-1lambda*4*-imidazo[2,1-b]thiazole
   Show/Hide
C18H14N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0404472
5-(4-Methanesulfonyl-phenyl)-3-methyl-6-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C19H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0406295
5-(4-Methanesulfonyl-phenyl)-6-phenyl-imidazo[2,1-b]thiazole-3-carboxylic acid ethyl ester
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C21H18N2O4S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0409180
6-(4-Methanesulfonyl-phenyl)-2-methyl-5-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C19H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0410010
6-(4-Methanesulfonyl-phenyl)-3-methyl-5-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C19H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0437670
5-(4-Methanesulfonyl-phenyl)-2,3-dimethyl-6-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C20H18N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0467337
6-(4-Methanesulfonyl-phenyl)-5-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C18H14N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0483637
2,3-Dichloro-6-(4-chloro-phenyl)-5-(4-methanesulfonyl-phenyl)-imidazo[2,1-b]thiazole
   Show/Hide
C18H11Cl3N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0492730
6-(3,4-Difluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-imidazo[2,1-b]thiazole
   Show/Hide
C18H12F2N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0494744
2-(4-Methanesulfonyl-phenyl)-3-phenyl-benzo[d]imidazo[2,1-b]thiazole
   Show/Hide
C22H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0502348
6-(4-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-imidazo[2,1-b]thiazole
   Show/Hide
C18H13FN2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0524161
3-(4-Methanesulfonyl-phenyl)-2-phenyl-benzo[d]imidazo[2,1-b]thiazole
   Show/Hide
C22H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0527628
5-(4-Methanesulfonyl-phenyl)-2-methyl-6-phenyl-imidazo[2,1-b]thiazole
   Show/Hide
C19H16N2O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0376342
5-(4-Methanesulfonyl-phenyl)-6-(3-methoxy-phenyl)-thiazolo[3,2-b][1,2,4]triazole
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C18H15N3O3S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0419384
5-(4-Methanesulfonyl-phenyl)-2-methyl-6-phenyl-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C18H15N3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0449756
6-(3-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-2-methyl-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C18H14FN3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0449757
6-(3-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C17H12FN3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0459216
6-(4-Methanesulfonyl-phenyl)-5-phenyl-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C17H13N3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0497173
6-(4-Methanesulfonyl-phenyl)-5-phenyl-thiazolo[2,3-c][1,2,4]triazole
   Show/Hide
C17H13N3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0505496
6-(3,5-Difluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-thiazolo[3,2-b][1,2,4]triazole
   Show/Hide
C17H11F2N3O2S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0379346
4-(4-Methanesulfonyl-phenyl)-5,5-dimethyl-3-phenylsulfanyl-5H-furan-2-one
   Show/Hide
C19H18O4S2
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0465037
4-(4-Methanesulfonyl-phenyl)-5,5-dimethyl-3-phenoxy-5H-furan-2-one
   Show/Hide
C19H18O5S
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0505182
3-Benzoyl-4-(4-methanesulfonyl-phenyl)-5,5-dimethyl-5H-furan-2-one
   Show/Hide
C20H18O5S
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0427144
3-[(5-cyano-3-fluoro)phenoxymethyl]-1-(4-methanesulfonylphenyl)-5-phenyl-1H-pyrazole
   Show/Hide
C24H18FN3O3S
 1
1
IC50 = 99560 nM
   TI
   LI
   LO
   TS
CP0341579
6-((3-fluoro-5-(4-methoxytetrahydro-2H-pyran-4-yl)phenoxy)methyl)-1-methylquinolin-2(1H)-one
   Show/Hide
C23H24FNO4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0428151
1-(4-methanesulfonylphenyl)-3-[(3-nitro)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C23H19N3O5S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0437318
1-(4-methanesulfonylphenyl)-3-[(3,4-dimethoxy)phenoxymethyl]-5-phenyl-1H-pyrazole
   Show/Hide
C25H24N2O5S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0511927
3-[(3-ethoxy)phenoxymethyl]-1-(4-methanesulfonylphenyl)-5-phenyl-1H-pyrazole
   Show/Hide
C25H24N2O4S
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0010057
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
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C19H16ClNO4
 26
1 Activity = 2.934682 nM
2 IC50 = 10 nM
3 IC50 = 12 nM
4 IC50 = 20 nM
5 IC50 = 40 nM
6 IC50 = 50 nM
7 IC50 = 51 nM
8 IC50 = 100 nM
9 IC50 = 110 nM
10 IC50 = 150 nM
11 IC50 = 180 nM
12 IC50 = 200 nM
13 IC50 = 220 nM
14 IC50 = 250 nM
15 IC50 = 260 nM
16 IC50 = 463.1 nM
17 IC50 = 750 nM
18 IC50 = 1200 nM
19 IC50 = 1400 nM
20 IC50 = 1560 nM
21 IC50 = 3870 nM
22 IC50 = 3900 nM
23 IC50 = 5600 nM
24 IC50 = 12500 nM
25 Ka = 185185.1852 nM
26 Kd = 253 nM
CP0008361
2-{2-[(2,6-dichlorophenyl)amino]phenyl}acetic acid
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C14H11Cl2NO2
 5
1 IC50 = 3 nM
2 IC50 = 12 nM
3 IC50 = 15 nM
4 IC50 = 70 nM
5 IC50 = 150 nM
CP0037366
5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
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C17H12ClF3N2O
 6
1 IC50 = 7 nM
2 IC50 = 7.8 nM
3 IC50 = 8.9 nM
4 IC50 = 9 nM
5 IC50 = 10 nM
6 IC50 = 53 nM
CP0011191
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzene-1-sulfonamide
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C17H14F3N3O2S
 42
1 IC50 = 125 nM
2 IC50 = 131.97 nM
3 IC50 = 300 nM
4 IC50 = 2600 nM
5 IC50 = 5330 nM
6 IC50 = 6120 nM
7 IC50 = 6130 nM
8 IC50 = 6300 nM
9 IC50 = 6650 nM
10 IC50 = 7000 nM
11 IC50 = 7700 nM
12 IC50 = 8000 nM
13 IC50 = 8750 nM
14 IC50 = 9200 nM
15 IC50 = 10000 nM
16 IC50 = 10700 nM
17 IC50 = 12470 nM
18 IC50 = 14000 nM
19 IC50 = 14200 nM
20 IC50 = 15000 nM
21 IC50 = 15030 nM
22 IC50 = 15275 nM
23 IC50 = 19880 nM
24 IC50 = 20400 nM
25 IC50 = 22900 nM
26 IC50 = 23000 nM
27 IC50 = 24300 nM
28 IC50 = 24470 nM
29 IC50 = 25390 nM
30 IC50 = 25740 nM
31 IC50 = 27000 nM
32 IC50 = 27500 nM
33 IC50 = 27830 nM
34 IC50 = 32600 nM
35 IC50 = 36440 nM
36 IC50 = 37310 nM
37 IC50 = 43370 nM
38 IC50 = 46890 nM
39 IC50 = 100000 nM
40 IC50 > 10000 nM
41 IC50 > 50000 nM
42 IC50 < 100000 nM
CP0105544
4-(3-fluorophenyl)-3-(4-methoxyphenyl)-2H-furan-5-one
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C17H13FO3
 1
1 IC50 = 480 nM
CP0061060
5-Bromo-2-(4-fluoro-phenyl)-3-(4-methanesulfonyl-phenyl)-thiophene
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C17H12BrFO2S2
 3
1 IC50 = 800 nM
2 IC50 = 810 nM
3 IC50 > 10000 nM
CP0090694
(E)-2'-des-methyl sulindac sulfide
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C19H15FO2S
 1
1 IC50 = 1800 nM
CP0045761
(S)-2-(4-Isobutyl-phenyl)-propionic acid
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C13H18O2
 1
1 IC50 = 2600 nM
CP0000036
(+-)-2-(p-isobutylphenyl)propionic acid
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C13H18O2
 7
1 IC50 = 2704 nM
2 IC50 = 3000 nM
3 IC50 = 6300 nM
4 IC50 = 6900 nM
5 IC50 = 11100 nM
6 IC50 = 18000 nM
7 IC50 = 25000 nM
CP0058319
2-Bromo-3-(4-fluoro-phenyl)-4-(4-methanesulfonyl-phenyl)-thiophene
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C17H12BrFO2S2
 1
1 IC50 = 5200 nM
CP0049684
5-(4-Fluoro-phenyl)-6-(4-methanesulfonyl-phenyl)-spiro[2.4]hept-5-ene
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C20H19FO2S
 1
1 IC50 = 5400 nM
CP0037144
4-(4-methanesulfonylphenyl)-3-phenyl-2,5-dihydrofuran-2-one
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C17H14O4S
 5
1 IC50 = 18800 nM
2 IC50 = 19000 nM
3 IC50 = 26000 nM
4 IC50 = 40000 nM
5 IC50 > 100000 nM
CP0189671
3-[1-(4-Acetyl-phenyl)-5-(4-methoxy-phenyl)-1H-pyrrol-2-yl]-propionic acid
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C22H21NO4
 1
1 IC50 = 25000 nM
CP0037213
(SC-57666)1-[2-(4-fluorophenyl)-1-cyclopentenyl]-4-methylsulfonylbenzene
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C18H17FO2S
 2
1 IC50 = 30000 nM
2 IC50 > 100000 nM
CP0040447
4-(5-methyl-3-phenyl-1,2-oxazol-4-yl)benzene-1-sulfonamide
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C16H14N2O3S
 1
1 IC50 = 34300 nM
CP0048346
N-[6-(2,4-difluorophenyl)sulfanyl-1-oxo-2,3-dihydroinden-5-yl]methanesulfonamide
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C16H13F2NO3S2
 2
1 IC50 > 10000 nM
2 IC50 > 100000 nM
CP0207407
4-(4-Fluoro-phenyl)-5-(4-methanesulfonyl-phenyl)-2-methyl-thiazole
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C17H14FNO2S2
 1
1 IC50 > 10000 nM
CP0517649
3-(4-Fluoro-phenyl)-2-(4-methanesulfonyl-phenyl)-6,7-dimethyl-pyrazolo[1,5-a]pyrimidine
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C21H18FN3O2S
 1
1 IC50 > 10000 nM
CP0014398
2-Hydroxybenzoate, I
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C7H6O3
 1
1 IC50 > 40000 nM
CP0132427
5-Chloro-3-(4-methanesulfonyl-phenyl)-6''-methyl-[2,3'']bipyridinyl
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C18H15ClN2O2S
 1
1 IC50 > 50000 nM
CP0228832
1-[5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)-6-(3,3,3-trifluoropropoxy)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C20H24F3NO6S
 1
1 IC50 > 50000 nM
CP0355875
1-[5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)-6-(4,4,4-trifluorobutoxy)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C21H26F3NO6S
 1
1 IC50 > 50000 nM
CP0363002
2-methyl-1-[5-methyl-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxypropan-2-ol
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C17H21NO4S
 1
1 IC50 > 50000 nM
CP0363003
1-[5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)-6-propan-2-yloxypyridin-2-yl]oxy-2-methylpropan-2-ol
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C20H27NO6S
 1
1 IC50 > 50000 nM
CP0365479
1-[6-butoxy-5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C21H29NO6S
 1
1 IC50 > 50000 nM
CP0365480
6-[6-butoxy-5-(hydroxymethyl)-2-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]pyridine-3-sulfonamide
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C19H27N3O6S
 1
1 IC50 > 50000 nM
CP0448757
1-[3-(4-Methanesulfonyl-phenyl)-5-trifluoromethyl-pyridin-2-yloxy]-2-methyl-propan-2-ol
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C17H18F3NO4S
 1
1 IC50 > 50000 nM
CP0559009
1-[5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C17H21NO5S
 1
1 IC50 > 50000 nM
CP0566352
1-[[6-butoxy-5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxymethyl]cyclobutan-1-ol
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C22H29NO6S
 1
1 IC50 > 50000 nM
CP0567483
1-[5-(hydroxymethyl)-6-(2-methoxyethoxy)-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C20H27NO7S
 1
1 IC50 > 50000 nM
CP0568029
1-[5-ethyl-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C18H23NO4S
 1
1 IC50 > 50000 nM
CP0570266
1-[5-(hydroxymethyl)-6-methoxy-3-(4-methylsulfonylphenyl)pyridin-2-yl]oxy-2-methylpropan-2-ol
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C18H23NO6S
 1
1 IC50 > 50000 nM
CP0570961
1-[5-(hydroxymethyl)-3-(4-methylsulfonylphenyl)-6-propoxypyridin-2-yl]oxy-2-methylpropan-2-ol
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C20H27NO6S
 1
1 IC50 > 50000 nM
CP0097394
5-(4-Fluoro-phenyl)-1-(4-methanesulfonyl-phenyl)-3-trifluoromethyl-1H-pyrazole
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C17H12F4N2O2S
 1
1 IC50 > 100000 nM
CP0195797
2-Bromo-4-(4-fluoro-phenyl)-3-(4-methanesulfonyl-phenyl)-thiophene
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C17H12BrFO2S2
 1
1 IC50 > 100000 nM
CP0244285
N-[1-oxo-6-(1,3-thiazol-2-ylsulfanyl)-2,3-dihydroinden-5-yl]methanesulfonamide
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C13H12N2O3S3
 1
1 IC50 > 100000 nM
CP0048985
5-(4-Fluoro-phenyl)-4-(4-methanesulfonyl-phenyl)-2-methyl-thiazole
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C17H14FNO2S2
 1
1 IC50 > 100000 nM
Clinical Information about the Protein
Target 1 ( Prostaglandin G/H synthase 1 (COX-1) )
Target Type Successful Target
Disease 19 Target-related Diseases  19
1 Pulmonary and extrapulmonary tuberculosis [ICD-11: 1B10.Z]
2 Inflammatory bowel disease [ICD-11: DD72]
3 Postoperative inflammation [ICD-11: 1A00-CA43.1]
4 Hypertriglyceridemia [ICD-11: 5C80.1]
5 Arthritis [ICD-11: FA20]
6 Dysmenorrhea [ICD-11: GA34.3]
7 Malnutrition [ICD-11: 5B50-5B71]
8 Ulcerative colitis [ICD-11: DD71]
9 Osteoarthritis [ICD-11: FA00-FA05]
10 Pain [ICD-11: MG30-MG3Z]
11 Seborrhoeic dermatitis [ICD-11: EA81]
12 Rheumatoid arthritis [ICD-11: FA20]
13 Miosis [ICD-11: LA11.62]
14 Myalgia [ICD-11: FB56.2]
15 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
16 Duchenne dystrophy [ICD-11: 8C70]
17 Gout [ICD-11: FA25]
18 Analgesia [ICD-11: MB40.8]
19 Giant cell arteritis [ICD-11: 4A44.2]
Approved Drug(s) 14 Approved Drugs  14
1 Aminosalicylic Acid Approved
Pulmonary and extrapulmonary tuberculosis
2 Balsalazide Approved
Inflammatory bowel disease
3 Bromfenac Approved
Postoperative inflammation
4 Eicosapentaenoic acid/docosa-hexaenoic acid Approved
Hypertriglyceridemia
5 FENBUFEN Approved
Arthritis
6 Flufenamic Acid Approved
Dysmenorrhea
7 Gamma-Homolinolenic acid Approved
Malnutrition
8 Meclofenamate Sodium Approved
Arthritis
9 Mesalazine Approved
Ulcerative colitis
10 Naproxen Approved
Osteoarthritis
11 Piroxicam Approved
Pain
12 Salicyclic acid Approved
Seborrhoeic dermatitis
13 Salsalate Approved
Rheumatoid arthritis
14 Suprofen Approved
Miosis
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 (S)-FLURBIPROFEN Preregistration
Myalgia
2 Curcumin Phase 3
Solid tumour/cancer
3 EPICATECHIN Phase 1/2
Duchenne dystrophy
4 Resveratrol Phase 3
Giant cell arteritis
Discontinued Drug(s) 4 Discontinued Drugs  4
1 INDOPROFEN Withdrawn from market
Gout
2 Metamizole Withdrawn from market
Pain
3 Phenacetin Withdrawn from market
Analgesia
4 TEBUFELONE Discontinued in Phase 2
Pain