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ChEMBL ligand: CHEMBL1956285 (Dsm265, Dsm-265, DSM265) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]