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Literature summary extracted from

  • Zhu, J.; Han, L.; Diao, Y.; Ren, X.; Xu, M.; Xu, L.; Li, S.; Li, Q.; Dong, D.; Huang, J.; Liu, X.; Zhao, Z.; Wang, R.; Zhu, L.; Xu, Y.; Qian, X.; Li, H.
    Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase (2015), J. Med. Chem., 58, 1123-1139.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.3.5.2 1-(2-((3,4-dimethylphenyl)amino)-4-methylthiazol-5-yl)-ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((3-chloro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((4-(tert-butyl)phenyl)amino)-4-methylthiazol-5-yl)-ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((4-bromophenyl)amino)-4-methylthiazol-5-yl)-ethanone
-
 Homo sapiens
1.3.5.2 1-(2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
-
 Homo sapiens
1.3.5.2 1-(2-(anthracen-2-ylamino)-4-methylthiazol-5-yl)ethan-1-one
-
 Homo sapiens
1.3.5.2 1-(4-methyl-2-(naphthalen-2-ylamino)thiazol-5-yl)ethan-1-one
-
 Homo sapiens
1.3.5.2 1-(4-methyl-2-(phenylamino)thiazol-5-yl)ethanone
-
 Homo sapiens
1.3.5.2 brequinar
-
 Homo sapiens
1.3.5.2 ethyl 2-((2,3-dihydro-1h-inden-5-yl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3,4-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3,4-dimethylphenyl)amino)-4-methylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3,4-dimethylphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3,5-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)-amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-chloro-4-((2-chloro-6-fluorobenzyl)oxy)phenyl)-amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-chloro-4-methylphenyl)amino)-4-cyclopropylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-chloro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-chloro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-chloro-4-phenoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((3-fluoro-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-(benzyloxy)-3-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-(tert-butyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-bromo-2-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-bromophenyl)amino)-4-methylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-(cyclopropanecarboxamido)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-((4-methoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-(anthracen-2-ylamino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-(benzo[d][1,3]dioxol-5-ylamino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-(naphthalen-2-ylamino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 2-([1,1'-biphenyl]-4-ylamino)-4-phenylthiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-(cyclopropanecarboxamido)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-(tert-butyl)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-(tert-butyl)-2-((3-chloro-4-methylphenyl)amino)-thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-(tert-butyl)-2-((3-fluoro-4-methylphenyl)amino)-thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-amino-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-amino-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-benzamido-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-benzamido-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-cyclopropyl-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-cyclopropyl-2-((4-fluoro-3-methylphenyl)amino)-thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-methyl-2-(naphthalen-2-ylamino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-phenyl-2-((4-(trifluoromethyl)phenyl)amino)-thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-phenyl-2-((5,6,7,8-tetrahydronaphthalen-2-yl)-amino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 ethyl 4-phenyl-2-(phenylamino)thiazole-5-carboxylate
-
 Homo sapiens
1.3.5.2 leflunomide
-
 Homo sapiens
1.3.5.2 teriflunomide
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining

Organism

EC Number Organism UniProt Comment Textmining
1.3.5.2 Homo sapiens Q02172
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.3.5.2 (S)-dihydroorotate + 2,6-dichlorophenolindophenol
-
 Homo sapiens orotate + reduced 2,6-dichlorophenolindophenol
-
 ?
1.3.5.2 (S)-dihydroorotate + decylubiquinone
-
 Homo sapiens orotate + reduced decylubiquinone
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.3.5.2 DHODH
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.3.5.2 FMN
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.3.5.2 0.000018
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-phenyl-2-((5,6,7,8-tetrahydronaphthalen-2-yl)-amino)thiazole-5-carboxylate
1.3.5.2 0.000026
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((2,3-dihydro-1h-inden-5-yl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000029
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-(naphthalen-2-ylamino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000035
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-chloro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000049
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000058
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3,4-dimethylphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000128
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000131
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000163
-
 at pH 8.0 and 22°C Homo sapiens teriflunomide
1.3.5.2 0.000174
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3,4-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000239
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000284
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-(tert-butyl)phenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000311
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3,5-difluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)-amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000325
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-cyclopropyl-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
1.3.5.2 0.000372
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-chloro-4-methylphenyl)amino)-4-cyclopropylthiazole-5-carboxylate
1.3.5.2 0.000393
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3,5-dichlorophenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000408
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-phenyl-2-((4-(trifluoromethyl)phenyl)amino)-thiazole-5-carboxylate
1.3.5.2 0.000453
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-(anthracen-2-ylamino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.000515
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-(tert-butyl)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
1.3.5.2 0.000552
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-(tert-butyl)-2-((3-chloro-4-methylphenyl)amino)-thiazole-5-carboxylate
1.3.5.2 0.000562
-
 at pH 8.0 and 22°C Homo sapiens 1-(4-methyl-2-(naphthalen-2-ylamino)thiazol-5-yl)ethan-1-one
1.3.5.2 0.000645
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-cyclopropyl-2-((4-fluoro-3-methylphenyl)amino)-thiazole-5-carboxylate
1.3.5.2 0.000652
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-(tert-butyl)-2-((3-fluoro-4-methylphenyl)amino)-thiazole-5-carboxylate
1.3.5.2 0.000784
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-phenyl-2-(phenylamino)thiazole-5-carboxylate
1.3.5.2 0.000887
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-methyl-2-(naphthalen-2-ylamino)thiazole-5-carboxylate
1.3.5.2 0.000969
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-chloro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
1.3.5.2 0.001108
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-(benzo[d][1,3]dioxol-5-ylamino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.001358
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3,4-dimethylphenyl)amino)-4-methylthiazole-5-carboxylate
1.3.5.2 0.00144
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-methoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.00193
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((4-bromo-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
1.3.5.2 0.001987
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazole-5-carboxylate
1.3.5.2 0.00211
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-amino-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
1.3.5.2 0.00235
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-methylthiazol-5-yl)ethanone
1.3.5.2 0.00365
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((4-(tert-butyl)phenyl)amino)-4-methylthiazol-5-yl)-ethanone
1.3.5.2 0.00385
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((3,4-dimethylphenyl)amino)-4-methylthiazol-5-yl)-ethanone
1.3.5.2 0.00394
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((3-chloro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
1.3.5.2 0.00604
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-chloro-3-(trifluoromethyl)phenyl)amino)-4-(cyclopropanecarboxamido)thiazole-5-carboxylate
1.3.5.2 0.00903
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-benzamido-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
1.3.5.2 0.00907
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-bromophenyl)amino)-4-methylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens 1-(4-methyl-2-(phenylamino)thiazol-5-yl)ethanone
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((4-bromophenyl)amino)-4-methylthiazol-5-yl)-ethanone
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-((3-fluoro-4-methylphenyl)amino)-4-methylthiazol-5-yl)ethanone
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens 1-(2-(anthracen-2-ylamino)-4-methylthiazol-5-yl)ethan-1-one
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-amino-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-(cyclopropanecarboxamido)-2-((3,4-dimethylphenyl)amino)thiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 4-benzamido-2-((4-chloro-3-(trifluoromethyl)phenyl)-amino)thiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-bromo-2-methylphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-([1,1'-biphenyl]-4-ylamino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-fluoro-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-chloro-4-phenoxyphenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((4-(benzyloxy)-3-chlorophenyl)amino)-4-phenylthiazole-5-carboxylate
1.3.5.2 0.01
-
 at pH 8.0 and 22°C Homo sapiens ethyl 2-((3-chloro-4-((2-chloro-6-fluorobenzyl)oxy)phenyl)-amino)-4-phenylthiazole-5-carboxylate