Target Validation Information
Target ID T60529
Target Name Prostaglandin G/H synthase 1
Target Type
Successful
Drug Potency against Target L-745337 Drug Info IC50 = 1600 nM [525423]
Suprofen Drug Info IC50 = 0.136 uM [553147]
2-Naphthalen-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 18000 nM [529474]
Prifelone Drug Info IC50 = 500 nM [527799]
2-Furan-2-ylmethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 13000 nM [529474]
2-Methyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 17000 nM [529474]
2-(3-Phenyl-propyl)-1,2-dihydro-indazol-3-one Drug Info IC50 = 3800 nM [529474]
2-(2-Methylpropanoyl)-1,3,5-benzenetriol Drug Info IC50 = 3800 nM [527829]
(11H-Dibenzo[b,e][1,4]dioxepin-2-yl)-acetic acid Drug Info IC50 = 100 nM [533456]
HONOKIOL Drug Info IC50 = 1800 nM [530176]
Mesalazine Drug Info IC50 = 50~1000 nM [552364]
1-(4-aminosulfonylphenyl)-2-(2-pyridyl)acetylene Drug Info IC50 = 9300 nM [529156]
1-(4-aminosulfonylphenyl)-2-(4-pyridyl)acetylene Drug Info IC50 = 3900 nM [529156]
CIMICOXIB Drug Info IC50 = 1900 nM [528708]
2-(3'-Vinyl-biphenyl-4-yl)-propionic acid Drug Info IC50 = 1300 nM [525446]
Acetic acid 2-hept-2-ynylsulfanyl-phenyl ester Drug Info IC50 = 17000 nM [534753]
TENIDAP Drug Info IC50 = 2560 nM [531252]
2-(3'-Allyl-biphenyl-4-yl)-propionic acid Drug Info IC50 = 1400 nM [525446]
5,3'-Dipropyl-biphenyl-2,4'-diol Drug Info IC50 = 800 nM [530176]
IODOINDOMETHACIN Drug Info IC50 = 780 nM [530753]
Icosapent Drug Info IC50 = 13000 nM [526089]
2,4'-Dimethoxy-5,3'-di-(2-propenyl)-biphenyl Drug Info IC50 = 11400 nM [530176]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiole-3-thione Drug Info IC50 = 30 nM [529881]
4,5-Bis(4-methoxyphenyl)-3H-1,2-dithiol-3-one Drug Info IC50 = 0.3 nM [529881]
5-(4-Chlorophenyl)-4-p-tolyl-1,2-selenazole Drug Info IC50 = 200 nM [529127]
5-(4-Chlorophenyl)-4-(4-methoxyphenyl)isothiazole Drug Info IC50 = 70 nM [529881]
Acetic acid 2-hexylsulfanyl-phenyl ester Drug Info IC50 = 8000 nM [534753]
4-(4-Chlorophenyl)-5-(4-methoxyphenyl)isothiazole Drug Info IC50 = 20 nM [529881]
2-(3'-Ethylsulfanyl-biphenyl-4-yl)-propionic acid Drug Info IC50 = 3100 nM [525446]
2-[4-(1H-Indol-5-yl)-phenyl]-propionic acid Drug Info IC50 = 100 nM [525446]
Acetic acid 2-hex-2-ynylsulfanyl-phenyl ester Drug Info IC50 = 14000 nM [534753]
2-(2-(2,6-dimethylphenylamino)phenyl)acetic acid Drug Info IC50 = 234 nM [528789]
1-(4-(methylsulfonyl)phenyl)-3-phenylurea Drug Info IC50 = 9200 nM [529273]
2-(3'-Ethyl-biphenyl-4-yl)-propionic acid Drug Info IC50 = 5800 nM [525446]
2-Phenethyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 15000 nM [529474]
4,5-Bis(4-methoxyphenyl)-1,2-selenazole Drug Info IC50 = 6 nM [529127]
4,5-Bis(4-methoxyphenyl)isothiazole Drug Info IC50 = 3 nM [529881]
2-(N-(2-Ffuorophenyl)pyrrol-3-yl) acetic acid Drug Info IC50 = 10600 nM [528854]
Acetic acid 2-heptylselanyl-phenyl ester Drug Info IC50 = 12000 nM [534753]
Acetic acid 2-pentylsulfanyl-phenyl ester Drug Info IC50 = 5000 nM [534753]
(11H-Dibenzo[b,e][1,4]dioxepin-8-yl)-acetic acid Drug Info IC50 = 10000 nM [533456]
4-(4-Chlorophenyl)-5-p-tolylisothiazole Drug Info IC50 = 200 nM [529881]
4-(5-(4-Hydroxyphenyl)isothiazol-4-yl)phenol Drug Info IC50 = 1000 nM [529881]
5-(4-Chlorophenyl)-4-p-tolylisothiazole Drug Info IC50 = 40 nM [529881]
5-(2-1H-indenyl)-1,3-benzodioxole Drug Info IC50 = 12800 nM [528934]
2-Benzyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 18000 nM [529474]
Acetic acid 2-hept-3-ynylsulfanyl-phenyl ester Drug Info IC50 = 18000 nM [534753]
N-(3-phenoxy-4-pyridinyl)ethanesulfonamide Drug Info IC50 = 5340 nM [527352]
4-amino-N-(4-chlorophenyl)benzenesulfonamide Drug Info IC50 = 12000 nM [528508]
N-(3-phenoxy-4-pyridinyl)propanesulfonamide Drug Info IC50 = 18360 nM [527352]
DOCOSAHEXAENOIC ACID Drug Info IC50 = 15000 nM [526089]
4-(4-Chlorophenyl)-5-p-tolyl-1,2-selenazole Drug Info IC50 = 50 nM [529127]
5-Methyl-3,4-diphenyl-isoxazole Drug Info IC50 = 90 nM [527215]
5-(4-Chlorophenyl)-4-p-tolyl-3H-1,2-dithiol-3-one Drug Info IC50 = 200 nM [529881]
4-(4-Chlorophenyl)-5-p-tolyl-3H-1,2-dithiol-3-one Drug Info IC50 = 20 nM [529881]
2-(2-methoxyphenyl)-1H-indene Drug Info IC50 = 460 nM [528934]
2-(p-Methylsulfonylbenzoyl)furan Drug Info IC50 = 15100 nM [531135]
2-Phenyl-1,2-dihydro-indazol-3-one Drug Info IC50 = 2700 nM [529474]
2-(2,3,4-trimethoxyphenyl)-1H-indene Drug Info IC50 = 30 nM [528934]
Oxametacin Drug Info IC50 = 2800 nM [529146]
N-(3-phenylamino-4-pyridinyl)methanesulfonamide Drug Info IC50 = 2260 nM [530415]
N-(3-phenoxypyridin-4-yl)methanesulfonamide Drug Info IC50 = 410 nM [530415]
2'-epi-guianin Drug Info IC50 = 18200 nM [530493]
PHENIDONE Drug Info IC50 = 3000 nM [529474]
5-Ethyl-3,4-diphenyl-isoxazole Drug Info IC50 = 50 nM [527215]
3 beta-O-acetyloleanolic acid Drug Info IC50 = 1 nM [528272]
(11H-Dibenzo[b,e][1,4]dioxepin-7-yl)-acetic acid Drug Info IC50 = 1400 nM [533456]
5-(2-Imidazol-1-yl-ethyl)-7,8-dihydro-quinoline Drug Info IC50 = 173 nM [525760]
1,2-dihydro-3-(2,3,4-trimethoxyphenyl)naphthalene Drug Info IC50 = 480 nM [528934]
1-(4-(methylsulfonyl)phenyl)-3-p-tolylurea Drug Info IC50 = 12500 nM [529273]
Salicyclic acid Drug Info IC50 = 1700 nM [552915]
IODOSUPROFEN Drug Info IC50 = 1000 nM [530753]
Alpha-Methyl-4-biphenyl-acetic acid Drug Info IC50 = 110 nM [530753]
N-(3-(phenylthio)pyridin-4-yl)methanesulfonamide Drug Info IC50 = 3620 nM [530415]
TEBUFELONE Drug Info IC50 = 250 nM [534599]
RESORCINOL Drug Info IC50 = 3600 nM [527310]
(Z)-2'-des-methyl sulindac sulfide Drug Info IC50 = 375 nM [530116]
4,5-Bis(4-chlorophenyl)-1,2-selenazole Drug Info IC50 = 200 nM [529127]
METHYLHONOKIOL Drug Info IC50 = 100 nM [530176]
4'-Methoxy-5,3'-dipropyl-biphenyl-2ol Drug Info IC50 = 7700 nM [530176]
4,5-Bis(4-chlorophenyl)isothiazole Drug Info IC50 = 100 nM [529881]
3-(4-Methanesulfonyl-phenyl)-1-phenyl-propynone Drug Info IC50 = 1000 nM [527727]
SC-58451 Drug Info IC50 = 140 nM
Primary alcohol metabolite of celecoxib Drug Info IC50 = 7100 nM [529754]
5-(4-Methoxyphenyl)-4-p-tolylisothiazole Drug Info IC50 = 10 nM [529881]
2-(N-(2-fluorophenyl)pyrrol-2-yl) acetic acid Drug Info IC50 = 19800 nM [528854]
Acetic acid 2-heptylsulfanyl-phenyl ester Drug Info IC50 = 6000 nM [534753]
5-(4-Methoxyphenyl)-4-p-tolyl-1,2-selenazole Drug Info IC50 = 20 nM [529127]
IMRECOXIB Drug Info IC50 = 115 nM [530021]
FENBUFEN Drug Info IC50 = 3900 nM [530153]
References
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Ref 529474J Med Chem. 1991 Mar;34(3):1028-36.Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.
Ref 529127Eur J Med Chem. 2008 Jun;43(6):1152-9. Epub 2007 Sep 22.Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
Ref 529881Bioorg Med Chem. 2009 Jan 15;17(2):558-68. Epub 2008 Dec 6.Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
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Ref 534753J Med Chem. 1998 Nov 19;41(24):4800-18.Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.
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Ref 533456J Med Chem. 1986 Aug;29(8):1436-41.Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids.
Ref 529881Bioorg Med Chem. 2009 Jan 15;17(2):558-68. Epub 2008 Dec 6.Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
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Ref 528934Bioorg Med Chem. 2007 Sep 15;15(18):6109-18. Epub 2007 Jun 20.'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.
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Ref 527215J Med Chem. 2004 Sep 23;47(20):4881-90.Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.
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Ref 533456J Med Chem. 1986 Aug;29(8):1436-41.Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids.
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Ref 529273Bioorg Med Chem Lett. 2008 Feb 15;18(4):1336-9. Epub 2008 Jan 11.Design and synthesis of 1,3-diarylurea derivatives as selective cyclooxygenase (COX-2) inhibitors.
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Ref 530753Bioorg Med Chem. 2010 Mar 15;18(6):2204-18. Epub 2010 Feb 8.In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
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Ref 530176Bioorg Med Chem. 2009 Jul 1;17(13):4459-65. Epub 2009 May 18.Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4-formation.
Ref 530176Bioorg Med Chem. 2009 Jul 1;17(13):4459-65. Epub 2009 May 18.Design and synthesis of ten biphenyl-neolignan derivatives and their in vitro inhibitory potency against cyclooxygenase-1/2 activity and 5-lipoxygenase-mediated LTB4-formation.
Ref 529881Bioorg Med Chem. 2009 Jan 15;17(2):558-68. Epub 2008 Dec 6.Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
Ref 527727Bioorg Med Chem Lett. 2005 Nov 1;15(21):4842-5.Synthesis and biological evaluation of 1,3-diphenylprop-2-yn-1-ones as dual inhibitors of cyclooxygenases and lipoxygenases.
Ref 529754Bioorg Med Chem. 2008 Nov 15;16(22):9694-8. Epub 2008 Oct 5.Diazen-1-ium-1,2-diolated nitric oxide donor ester prodrugs of 5-(4-hydroxymethylphenyl)-1-(4-aminosulfonylphenyl)-3-trifluoromethyl-1H-pyrazole and its methanesulfonyl analog: synthesis, biological evaluation and nitric oxide release studies.
Ref 529881Bioorg Med Chem. 2009 Jan 15;17(2):558-68. Epub 2008 Dec 6.Diaryl-dithiolanes and -isothiazoles: COX-1/COX-2 and 5-LOX-inhibitory, *OH scavenging and anti-adhesive activities.
Ref 528854Bioorg Med Chem. 2007 Jul 15;15(14):4876-90. Epub 2007 May 3.Synthesis and biological activity of new anti-inflammatory compounds containing the 1,4-benzodioxine and/or pyrrole system.
Ref 534753J Med Chem. 1998 Nov 19;41(24):4800-18.Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.
Ref 529127Eur J Med Chem. 2008 Jun;43(6):1152-9. Epub 2007 Sep 22.Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles.
Ref 530021Bioorg Med Chem Lett. 2009 Apr 15;19(8):2270-2. Epub 2009 Feb 27.Synthesis and anti-inflammatory activity of the major metabolites of imrecoxib.
Ref 530153Eur J Med Chem. 2009 Sep;44(9):3798-804. Epub 2009 Apr 14.Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents.

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