DSM265 [Ligand Id: 9644] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1956285 (Dsm-265, Dsm265, DSM265) |
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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] |
| dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2991] [GtoPdb: 2604] [UniProtKB: O35435] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged mouse DHODH expressed in Escherichia coli BL21 using L-DHO as substrate and CoQ as co-substrate by DCIP dye based spectrophotometric assay | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2016) 59: 5416-5431 [PMID:27127993] |
| dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2383] [GtoPdb: 2604] [UniProtKB: Q63707] | ||||||||
| ChEMBL | Inhibition of N-terminal His6-tagged rat DHODH expressed in Escherichia coli BL21 expressed in Escherichia coli BL21 using L-DHO as substrate and CoQ as co-substrate by DCIP dye based spectrophotometric assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2016) 59: 5416-5431 [PMID:27127993] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG by patch clamp electrophysiology assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2016) 59: 5416-5431 [PMID:27127993] |
| ChEMBL | Inhibition of human ERG by IonWorks patch clamp electrophysiology assay | B | 5.15 | pEC50 | 7000 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Inhibition of human ERG by patch clamp assay | B | 5.8 | pEC50 | 1600 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| 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 R1AC1B harboring DHODH C276F mutant measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 6.77 | pEC50 | 170 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum R10C1B harboring DHODH G181C mutant measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 6.92 | pEC50 | 120 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| 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 Plasmodium falciparum R1BC1A harboring DHODH L531F mutant measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum R2B harboring DHODH R265G mutant measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 7.13 | pEC50 | 74 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| 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 Plasmodium falciparum 1D3 measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| 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 | F | 8.11 | pEC50 | 7.8 | nM | EC50 | J Med Chem (2019) 62: 10526-10562 [PMID:31385706] |
| 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 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] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 infected in human red blood cells after 72 hrs by SYBR Green 1 dye based fluorescence assay | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D70087/N9 infected in po dosed NOD-SCID IL2Rgamma null mouse assessed as reduction in parasitemia administered once daily for 4 days by flow cytometric analysis | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum Dd2 measured after 72 hrs by SYBR Green dye based fluorescence assay | F | 8.34 | pEC50 | 4.6 | nM | EC50 | J Med Chem (2020) 63: 4929-4956 [PMID:32248693] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBC assessed as reduction in parasitemia incubated for 72 hrs by SYBR green dye-based assay | F | 8.37 | pEC50 | 4.3 | nM | EC50 | J Med Chem (2016) 59: 5416-5431 [PMID:27127993] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
