1.3.98.1 1,5-dihydrofuro[3,4-d]pyrimidine-2,4,7-trione - 163089 1.3.98.1 1-(1-naphthyl)-3-[2-(trifluoromethyl)phenyl]urea 50% inhibition at 0.0004 mM, wild type, 0.00034 mM, mutant R265A, above 0.2, mutant H185A 55757 1.3.98.1 1-(2-methoxyphenyl)-3-(1-naphthyl)urea 50% inhibition at 0.00023 mM, wild type, 0.00024 mM, mutant R265A, 0.140, mutant H185A 55758 1.3.98.1 1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(4-methyl-benzylamide) 5-phenylamide minimum inhibitory concentration 0.032 mg/ml 23022 1.3.98.1 1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-(isobutyl-amide) minimum inhibitory concentration above 0.064 mg/ml 23020 1.3.98.1 1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[(4-carbamoyl-phenyl)-amide] minimum inhibitory concentration 0.008 mg/ml 23016 1.3.98.1 1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.00025 mg/ml 23021 1.3.98.1 1-(4-Chloro-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[(4-piperidin-1-yl-phenyl)-amide] 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.002 mg/ml 23019 1.3.98.1 1-(4-chlorophenyl)-3-quinolin-8-ylurea 50% inhibition at 0.00078 mM, wild type, 0.002 mM, mutant R265A, above 0.4, mutant H185A 55759 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-(isobutyl-amide) 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration 0.064 mg/ml 23015 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzhydryl-amide 5-benzylamide minimum inhibitory concentration above 0.032 mg/ml 23014 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 3-benzylamide 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration 0.003 mg/ml 23012 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-benzylamide 3-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] minimum inhibitory concentration above 0.032 mg/ml 23013 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-phenylamide 3-[(pyridin-3-ylmethyl)-amide] minimum inhibitory concentration 0.0005 mg/ml 23023 1.3.98.1 1-(4-Methoxy-phenyl)-1H-pyrazole-3,5-dicarboxylic acid 5-[[4-(pyrrolidine-1-carbonyl)-phenyl]-amide] 3-[(tetrahydro-furan-2-yl)-amide] minimum inhibitory concentration above 0.032 mg/ml 23017 1.3.98.1 2,3-dihydrotriazolo[4,5-d]pyrimidine-5,7-dione - 163084 1.3.98.1 2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid - 163082 1.3.98.1 2-methyl-3-nitro-N-[3-(trifluoromethyl)phenyl]benzamide 50% inhibition at 0.00008 mM, wild type, 0.00037 mM, mutant R265A, 0.120, mutant H185A 55756 1.3.98.1 2-methyl-N-1-naphthyl-3-nitrobenzamide 50% inhibition at 0.00008 mM, wild type, 0.00048 mM, mutant R265A, 0.180, mutant H185A 55754 1.3.98.1 2-thioorotate orotate analogue, 50% inhibition at 0.018 mM 108171 1.3.98.1 3,4-dihydroxybenzoate - 736 1.3.98.1 3,4-dihydroxybenzoate competitive inhibition at 1 mM 736 1.3.98.1 3,5-Dihydroxybenzoate - 5904 1.3.98.1 3,5-Dihydroxybenzoate non-competitive inhibition at 1 mM 5904 1.3.98.1 4,6-dioxo-1,4,5,6-tetrahydro-1,3,5-triazine-2-carboxylic acid - 163083 1.3.98.1 5-amino-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid - 163085 1.3.98.1 5-aminoorotate orotate analogue, 50% inhibition at 1.6 mM 8385 1.3.98.1 5-bromoorotate orotate analogue, 50% inhibition at 0.016 mM 8387 1.3.98.1 5-fluoro-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid - 163087 1.3.98.1 5-Fluoroorotate orotate analogue, 50% inhibition at 0.055 mM 3183 1.3.98.1 5-nitro-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid - 163086 1.3.98.1 5-nitroorotate orotate analogue, 50% inhibition at 0.076 mM 108536 1.3.98.1 5-[(dimethylamino)methyl]-2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid - 163091 1.3.98.1 7,9-dihydro-3H-purine-2,6,8-trione - 163088 1.3.98.1 Barbiturate dead-end inhibitor, competitive with respect to (S)-dihydroorotate 5522 1.3.98.1 butyl 2,6-dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylate - 163090 1.3.98.1 HgCl2 - 110 1.3.98.1 L-orotate - 68893 1.3.98.1 leflunomide cell line A20R resistant to leflunomide shows enhanced expression of enzyme to bypass the inhibitory effect, following long-time exposure, enzyme gene amplification can be assumed 8448 1.3.98.1 Mercuric chloride 40% inhibition after 15 min at 0.000045 mM 5577 1.3.98.1 methanol extract of brown algae Fucus evanescens 59% inhibition, noncompetitive 123001 1.3.98.1 methanol extract of brown algae Pelvetia babingtonii 58% inhibition, noncompetitive 123002 1.3.98.1 additional information markable sensitivity to sulfhydryl inhibitors 2 1.3.98.1 additional information visible light is inactivating 2 1.3.98.1 additional information brequinar and DPC-AE661100 have no effect, even at a concentration of 1 mM 2 1.3.98.1 additional information inhibitor virtual screening, overview 2 1.3.98.1 N-(2,4-dichlorophenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00008 mM, mutant R265A, above 0.05, mutant H185A 55749 1.3.98.1 N-(2-fluorophenyl)naphthalene-2-carboxamide 50% inhibition at 0.00047 mM, wild type, 0.00030 mM, mutant R265A, 0.21, mutant H185A 123000 1.3.98.1 N-(3,4-dichlorophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00008 mM, wild type, 0.0028 mM, mutant R265A, 0.06, mutant H185A 55755 1.3.98.1 N-(3,4-difluorophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00026 mM, wild type, 0.00082 mM, mutant R265A, 0.25, mutant H185A 55753 1.3.98.1 N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00002 mM, wild type, 0.0004 mM, mutant R265A, 0.13, mutant H185A 13654 1.3.98.1 N-(3-bromophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.00006 mM, wild type, 0.0012 mM, mutant R265A, 0.140, mutant H185A 55751 1.3.98.1 N-(3-chloro-4-fluorophenyl)-2-methyl-3-nitrobenzamide 50% inhibition at 0.0001 mM, wild type, 0.0005 mM, mutant R265A, 0.13, mutant H185A 55752 1.3.98.1 N-(4-bromo-2-methylphenyl)-2-naphthamide 50% inhibition at 0.00005 mM, wild type, 0.00005 mM, mutant R265A, 0.57, mutant H185A 55750 1.3.98.1 N-ethylmaleimide - 49 1.3.98.1 N3-benzyl-1-(4-chlorophenyl)-N5-phenyl-1H-pyrazole-3,5-dicarboxamide minimum inhibitory concentration 0.000125 mg/ml 23018 1.3.98.1 Orotate competitive to dihydroorotate in ferricyanide reduction assay 446 1.3.98.1 Orotate - 446 1.3.98.1 Orotate competitive, with ferricyanide as electron acceptor 446 1.3.98.1 Orotate competitive product inhibition 446 1.3.98.1 Orotate competitive 446 1.3.98.1 Orotate competitively inhibits all three DHOD enzymes to a comparable level 446 1.3.98.1 orotate methyl ester orotate analogue, 50% inhibition at 0.71 mM 107617 1.3.98.1 oxonate crystallization data 6157 1.3.98.1 oxonic acid orotate analogue, 50% inhibition at 0.0099 mM 109380 1.3.98.1 p-hydroxymercuribenzoate 98% inhibition after 5 min at 0.00227 mM 98 1.3.98.1 Salicylhydroxamic acid weak inhibition, pH 9.0, 37°C 2501 1.3.98.1 suramin weak inhibition, pH 9.0, 37°C 704 1.3.98.1 Tiron inhibits cytochrome c reduction and sulfite autoxidation 1881 1.3.98.1 Uracil orotate analogue, 50% inhibition at 2.5 mM 334