DSM265 [Ligand Id: 9644] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1956285 (Dsm265, Dsm-265, DSM265)
  • Dihydroorotate dehydrogenase in Plasmodium falciparum [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
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  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
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  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum NF54 [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium vivax [GtoPdb: 2949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dihydroorotate dehydrogenase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3486] [UniProtKB: Q54A96]
ChEMBL Inhibition of Plasmodium falciparum C-terminal hexa-His tagged DHODH expressed in Escherichia coli by DCIP reduction assay B 7.48 pIC50 33 nM IC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Inhibition of Plasmodium falciparum DHODH expressed in Escherichia coli using L-dihydroorotate as substrate B 8 pIC50 10 nM IC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
ChEMBL Inhibition of human C-terminal hexa-His tagged DHODH expressed in Escherichia coli by DCIP reduction assay B 4 pIC50 >100000 nM IC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Inhibition of human DHODH expressed in Escherichia coli by DCIP staining-based spectrophotometric analysis B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2019) 165: 332-346 [PMID:30703745]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum Dd2 harboring DHODH mutant F 6.98 pIC50 104 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against wild type Plasmodium falciparum Dd2 F 8.37 pIC50 4.3 nM IC50 J Med Chem (2018) 61: 4213-4227 [PMID:29665687]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 transfected with yeast DHODH by [3H]hypoxanthine incorporation assay F 4.7 pEC50 >20000 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against schizont stage of Plasmodium falciparum clinical isolate F 6.04 pEC50 918 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against Plasmodium falciparum D10 by [3H]hypoxanthine incorporation assay F 7.07 pEC50 86 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 by [3H]hypoxanthine incorporation assay in presence of human serum F 7.24 pEC50 57 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay in presence of human serum F 7.34 pEC50 46 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against atovoquone-resistant Plasmodium falciparum TM90C2A by [3H]hypoxanthine incorporation assay in presence of human serum F 7.51 pEC50 31 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against drug-sensitive Plasmodium falciparum HB3 by [3H]hypoxanthine incorporation assay in presence of human serum F 7.57 pEC50 27 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against drug-sensitive Plasmodium falciparum D6 by [3H]hypoxanthine incorporation assay in presence of human serum F 7.66 pEC50 22 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against atovoquone-resistant Plasmodium falciparum TM90C2B by [3H]hypoxanthine incorporation assay in presence of human serum F 7.82 pEC50 15 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 by [3H]hypoxanthine incorporation assay in presence of albumax F 8.11 pEC50 7.8 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 F 8.11 pEC50 7.8 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against mefloquine/chloroquine-resistant Plasmodium falciparum asexual blood stage forms F 8.15 pEC50 7 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay in presence of human serum F 7.24 pEC50 57 nM EC50 J. Med. Chem. (2011) 54: 5540-5561 [PMID:21696174]
Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013]
ChEMBL Antimalarial activity against Plasmodium vivax infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation incubated for 40 hrs followed by addition of [3H]-hypoxanthine and measured after 4 hrs by liquid scintillation counting method F 6.28 pEC50 529 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
ChEMBL Antimalarial activity against schizont stage of Plasmodium vivax clinical isolate F 6.72 pEC50 190 nM EC50 J Med Chem (2019) 62: 10526-10562 [PMID:31385706]
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum [GtoPdb: 2949]
GtoPdb Steady-state kinetic analysis. - 7.52 pIC50 30 nM IC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum NF54 [GtoPdb: 2949]
GtoPdb Parasite growth inhibition assay - 7.52 pIC50 30 nM IC50 Sci Transl Med (2015) 7: 296ra111 [PMID:26180101]
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium vivax [GtoPdb: 2949]
GtoPdb Steady-state kinetic analysis. - 7.14 pIC50 72 nM IC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]