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Prostaglandin G/H synthase 2
A prostaglandin G/H synthase 2 that is encoded in the genome of rat. [OMA:P35355, PRO:DNx]
Synonyms
EC 1.14.99.1;
Cyclooxygenase-2;
COX-2;
PHS II;
Prostaglandin H2 synthase 2;
PGH synthase 2;
PGHS-2;
Prostaglandin-endoperoxide synthase 2
Research
Bioassay Publications (30)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 8 (26.67) | 18.7374 |
| 1990's | 16 (53.33) | 18.2507 |
| 2000's | 2 (6.67) | 29.6817 |
| 2010's | 4 (13.33) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (41)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| celecoxib | Rattus norvegicus (Norway rat) | IC50 | 0.4028 | 4 | 4 |
| diclofenac | Rattus norvegicus (Norway rat) | IC50 | 0.5000 | 1 | 1 |
| ibuprofen | Rattus norvegicus (Norway rat) | IC50 | 1.3000 | 2 | 2 |
| indomethacin | Rattus norvegicus (Norway rat) | IC50 | 0.5504 | 7 | 7 |
| ly 171883 | Rattus norvegicus (Norway rat) | IC50 | 44.0000 | 1 | 1 |
| meclofenamic acid | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 2 | 2 |
| meclofenamate sodium anhydrous | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 3 | 3 |
| masoprocol | Rattus norvegicus (Norway rat) | IC50 | 40.0000 | 2 | 2 |
| phenylbutazone | Rattus norvegicus (Norway rat) | IC50 | 15.0000 | 1 | 1 |
| pf 5901 | Rattus norvegicus (Norway rat) | IC50 | 300.0000 | 1 | 1 |
| rofecoxib | Rattus norvegicus (Norway rat) | IC50 | 0.7600 | 1 | 1 |
| phenidone | Rattus norvegicus (Norway rat) | IC50 | 8.0000 | 2 | 2 |
| acridan | Rattus norvegicus (Norway rat) | IC50 | 1.9000 | 1 | 1 |
| phenothiazine | Rattus norvegicus (Norway rat) | IC50 | 0.9400 | 1 | 1 |
| oxamethacin | Rattus norvegicus (Norway rat) | IC50 | 1.1000 | 1 | 1 |
| nafazatrom | Rattus norvegicus (Norway rat) | IC50 | 75.0000 | 2 | 2 |
| bw-755c | Rattus norvegicus (Norway rat) | IC50 | 5.5000 | 2 | 2 |
| 2-(5-ethylpyridin-2-yl)benzimidazole | Rattus norvegicus (Norway rat) | IC50 | 76.0000 | 1 | 1 |
| dazoxiben | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| pravadoline | Rattus norvegicus (Norway rat) | IC50 | 30.0000 | 1 | 1 |
| tepoxalin | Rattus norvegicus (Norway rat) | IC50 | 3.5250 | 2 | 2 |
| wy 48252 | Rattus norvegicus (Norway rat) | IC50 | 6.2000 | 2 | 2 |
| tenidap | Rattus norvegicus (Norway rat) | IC50 | 0.0315 | 2 | 2 |
| phenoxazine | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| 2(3h)-benzofuranone | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| ibuproxam | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| 1-benzyl-1h-indazol-3-ol | Rattus norvegicus (Norway rat) | IC50 | 31.0000 | 1 | 1 |
| 3-indazolinone | Rattus norvegicus (Norway rat) | IC50 | 30.0000 | 1 | 1 |
| sr 2640 | Rattus norvegicus (Norway rat) | IC50 | 2.0000 | 1 | 1 |
| wy 45911 | Rattus norvegicus (Norway rat) | IC50 | 40.1333 | 3 | 3 |
| rg 6866 | Rattus norvegicus (Norway rat) | IC50 | 9.5000 | 2 | 2 |
| nepafenac | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| naproxen | Rattus norvegicus (Norway rat) | IC50 | 0.0600 | 1 | 1 |
| quercetin | Rattus norvegicus (Norway rat) | IC50 | 50.0000 | 2 | 2 |
| baicalein | Rattus norvegicus (Norway rat) | IC50 | 50.0000 | 1 | 1 |
| e 5110 | Rattus norvegicus (Norway rat) | IC50 | 0.3600 | 3 | 3 |
| kme 4 | Rattus norvegicus (Norway rat) | IC50 | 1.3625 | 4 | 4 |
| ci 987 | Rattus norvegicus (Norway rat) | IC50 | 0.3500 | 1 | 1 |
| ahr 5850 | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
| piroxicam | Rattus norvegicus (Norway rat) | IC50 | 0.1000 | 1 | 1 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ibuprofen | Rattus norvegicus (Norway rat) | Change | 0.6000 | 1 | 1 |
| bw-755c | Rattus norvegicus (Norway rat) | Change | 6.0000 | 2 | 2 |
| zileuton | Rattus norvegicus (Norway rat) | Change | 16.0000 | 1 | 1 |
| naproxen | Rattus norvegicus (Norway rat) | Change | 0.2000 | 2 | 2 |
Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Design, synthesis and bioactivities of Celecoxib analogues or derivatives.Bioorganic & medicinal chemistry, , 09-01, Volume: 25, Issue:17, 2017
Discovery of novel hybrids of diaryl-1,2,4-triazoles and caffeic acid as dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase for cancer therapy.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group.ACS medicinal chemistry letters, , Aug-10, Volume: 8, Issue:8, 2017
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
Discovery of new indomethacin-based analogs with potentially selective cyclooxygenase-2 inhibition and observed diminishing to PGE2 activities.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-22, Volume: 11, Issue:20, 2001
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
Antiinflammatory agents. 4. Syntheses and biological evaluation of potential prodrugs of 2-amino-3-benzoylbenzeneacetic acid and 2-amino-3-(4-chlorobenzoyl)benzeneacetic acid.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
Differential effects of a series of hydroxamic acid derivatives on 5-lipoxygenase and cyclooxygenase from neutrophils and 12-lipoxygenase from platelets and their in vivo effects on inflammation and anaphylaxis.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
2,3-Dihydrobenzofuran-2-ones: a new class of highly potent antiinflammatory agents.Journal of medicinal chemistry, , Volume: 24, Issue:12, 1981
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.Journal of medicinal chemistry, , Apr-16, Volume: 36, Issue:8, 1993
1,3,4-Oxadiazole, 1,3,4-thiadiazole, and 1,2,4-triazole analogs of the fenamates: in vitro inhibition of cyclooxygenase and 5-lipoxygenase activities.Journal of medicinal chemistry, , Jun-25, Volume: 36, Issue:13, 1993
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.Journal of medicinal chemistry, , Oct-02, Volume: 35, Issue:20, 1992
Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.Journal of medicinal chemistry, , Volume: 33, Issue:8, 1990
5-Lipoxygenase inhibitors: synthesis and structure-activity relationships of a series of 1-aryl-2H,4H-tetrahydro-1,2,4-triazin-3-ones.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Indazolinones, a new series of redox-active 5-lipoxygenase inhibitors with built-in selectivity and oral activity.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
N-[(arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene D4 antagonists of novel structure.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
1,2-Dihydro-1-oxopyrrolo[3,2,1-kl]phenothiazine-2-carboxamides and congeners, dual cyclooxygenase/5-lipoxygenase inhibitors with antiinflammatory activity.Journal of medicinal chemistry, , Volume: 33, Issue:7, 1990
N-[(arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.Journal of medicinal chemistry, , Volume: 30, Issue:2, 1987
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Volume: 29, Issue:8, 1986
Synthesis and antiinflammatory activity of certain 5,6,7,8-tetrahydroquinolines and related compounds.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Antiinflammatory activity of substituted 6-hydroxypyrimido[2,1-f]purine-2,4,8(1H,3H,9H)-triones. Atypical nonsteroidal antiinflammatory agents.Journal of medicinal chemistry, , Volume: 29, Issue:6, 1986
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.Journal of medicinal chemistry, , Apr-16, Volume: 36, Issue:8, 1993
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.Journal of medicinal chemistry, , Jan-21, Volume: 37, Issue:2, 1994
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.Journal of medicinal chemistry, , Apr-16, Volume: 36, Issue:8, 1993
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.Journal of medicinal chemistry, , Volume: 34, Issue:2, 1991
Penta- and hexadienoic acid derivatives: a novel series of 5-lipoxygenase inhibitors.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990