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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
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]
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]
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 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]
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 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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]