Target Validation Information
Target ID T01318
Target Name Dihydroorotate dehydrogenase, mitochondrial
Target Type
Successful
Drug Potency against Target N-(Biphenyl-4-yl)-2-cyano-3-hydroxybut-2-enamide Drug Info IC50 = 90 nM [530060]
2-(3-(3,5-dichlorophenyl)ureido)benzoic acid Drug Info IC50 = 700 nM [530724]
BREQUINAR Drug Info IC50 = 3 nM [530724]
N-(3,5-dichlorophenyl)-2-methyl-3-nitrobenzamide Drug Info Ki = 30 nM [528617]
Ethyl 3-(biphenyl-3-ylamino)-2-cyanoacrylate Drug Info Ki = 2.45 nM [528617]
3-hydroxy-2-phenylquinoline-4-carboxylic acid Drug Info IC50 = 12000 nM [528605]
Diethyl 2-((biphenyl-3-ylamino)methylene)malonate Drug Info Ki = 10000 nM [528617]
GNF-PF-85 Drug Info IC50 = 330 nM [529511]
N-(4-bromo-2-methylphenyl)-2-naphthamide Drug Info Ki = 20 nM [528617]
2-(2-naphthamido)benzoic acid Drug Info IC50 = 13800 nM [527807]
1-hydroxy-2-dodecyl-4(1H)quinolone Drug Info IC50 = 4000 nM [529879]
2-(2-bromo-2-naphthamido)benzoic acid Drug Info IC50 = 8400 nM [527807]
2-[(biphenyl-4-carbonyl)-amino]-benzoic acid Drug Info IC50 = 5000 nM [527807]
Action against Disease Model Atovaquone The synergistic potential of a range of biguanides, their triazine metabolites, tetracyclines, and pyrimethamine in combination with atovaquone has been assessed. All five biguanides tested interacted synergistically with atovaquone against Plasmodi uM falcipar uM in vitro. All of the other compounds tested were either additive or antagonistic.IC50 on Plasmodi uM falcipar uMin vitro: 0.9nM [552301] Drug Info
References
Ref 552301Biguanide-atovaquone synergy against Plasmodium falciparum in vitro. Antimicrob Agents Chemother. 2002 Aug;46(8):2700-3.
Ref 530060J Med Chem. 2009 May 14;52(9):2683-93.Structure-based design, synthesis, and characterization of inhibitors of human and Plasmodium falciparum dihydroorotate dehydrogenases.
Ref 530724Bioorg Med Chem Lett. 2010 Mar 15;20(6):1981-4. Epub 2010 Jan 25.Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures.
Ref 530724Bioorg Med Chem Lett. 2010 Mar 15;20(6):1981-4. Epub 2010 Jan 25.Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures.
Ref 528617J Med Chem. 2007 Jan 25;50(2):186-91.Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
Ref 528617J Med Chem. 2007 Jan 25;50(2):186-91.Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
Ref 528605J Med Chem. 2007 Jan 11;50(1):21-39.Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.
Ref 528617J Med Chem. 2007 Jan 25;50(2):186-91.Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
Ref 529511J Med Chem. 2008 Jun 26;51(12):3649-53. Epub 2008 Jun 4.Triazolopyrimidine-based dihydroorotate dehydrogenase inhibitors with potent and selective activity against the malaria parasite Plasmodium falciparum.
Ref 528617J Med Chem. 2007 Jan 25;50(2):186-91.Design and synthesis of potent inhibitors of the malaria parasite dihydroorotate dehydrogenase.
Ref 527807Bioorg Med Chem Lett. 2006 Jan 1;16(1):88-92. Epub 2005 Oct 19.The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
Ref 529879Bioorg Med Chem Lett. 2009 Feb 1;19(3):972-5. Epub 2008 Nov 24.Type II NADH dehydrogenase of the respiratory chain of Plasmodium falciparum and its inhibitors.
Ref 527807Bioorg Med Chem Lett. 2006 Jan 1;16(1):88-92. Epub 2005 Oct 19.The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.
Ref 527807Bioorg Med Chem Lett. 2006 Jan 1;16(1):88-92. Epub 2005 Oct 19.The first de novo designed inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.

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