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Literature summary extracted from

  • Kuklish, S.L.; Antonysamy, S.; Bhattachar, S.N.; Chandrasekhar, S.; Fisher, M.J.; Fretland, A.J.; Gooding, K.; Harvey, A.; Hughes, N.E.; Luz, J.G.; Manninen, P.R.; McGee, J.E.; Navarro, A.; Norman, B.H.; Partridge, K.M.; Quimby, S.J.; Schiffler, M.A.; Sloan, A.V.; Warshawsky, A.M.; York, J.S.; Yu, X.P.
    Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors (2016), Bioorg. Med. Chem. Lett., 26, 4824-4828 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.99.3 (4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 (4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
-
 Homo sapiens
5.3.99.3 1-[6-(4-chlorophenyl)-5-methyl-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
-
 Homo sapiens
5.3.99.3 2-(difluoromethyl)-5-[(2-methylpropanamido)methyl]-N-[5-methyl-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-2-yl]pyridine-3-carboxamide
-
 Homo sapiens
5.3.99.3 2-methyl-2-(cis-4-[[1-(3-methyl-5-phenylfuro[2,3-b]pyridin-6-yl)piperidine-4-carbonyl]amino]cyclohexyl)propanoic acid
-
 Homo sapiens
5.3.99.3 N-cyclopentyl-1-[5,6-diamino-1-(3-amino-4-fluorophenyl)-1H-benzimidazol-2-yl]piperidine-4-carboxamide
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
5.3.99.3 microsome
-
 Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
5.3.99.3 Prostaglandin H2 Homo sapiens
-
 Prostaglandin E2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
5.3.99.3 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.99.3 Prostaglandin H2
-
 Homo sapiens Prostaglandin E2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.99.3 microsomal prostaglandin E synthase-1
-
 Homo sapiens
5.3.99.3 mPGES-1
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens (4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
5.3.99.3 0.000001
-
 pH and temperature not specified in the publication Homo sapiens (4S)-N-[(3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
5.3.99.3 0.000002
-
 pH and temperature not specified in the publication Homo sapiens 1,5-anhydro-2,3,4-trideoxy-3-[[(4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)piperidine-4-carbonyl]amino]-D-glycero-hexitol
5.3.99.3 0.000003
-
 pH and temperature not specified in the publication Homo sapiens (4S)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
5.3.99.3 0.000004
-
 pH and temperature not specified in the publication Homo sapiens (4S)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide
5.3.99.3 0.000006
-
 pH and temperature not specified in the publication Homo sapiens (4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxolan-3-yl]piperidine-4-carboxamide
5.3.99.3 0.000007
-
 pH and temperature not specified in the publication Homo sapiens (4S)-3,3-dimethyl-1-(8-methylquinolin-2-yl)-N-[(3S)-oxan-3-yl]piperidine-4-carboxamide
5.3.99.3 0.000012
-
 pH and temperature not specified in the publication Homo sapiens (4S)-3,3-dimethyl-N-(3-methylbutan-2-yl)-1-(8-methylquinolin-2-yl)piperidine-4-carboxamide
5.3.99.3 0.000504
-
 pH and temperature not specified in the publication Homo sapiens (4R)-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-3,3-dimethyl-1-[4-(trifluoromethyl)phenyl]piperidine-4-carboxamide
5.3.99.3 0.00372
-
 pH and temperature not specified in the publication Homo sapiens (4R)-1-(8-chloroquinolin-2-yl)-N-[cis-4-(hydroxymethyl)cyclohexyl]-3,3-dimethylpiperidine-4-carboxamide