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 K1 | F | 8.59 | pIC50 | 2.6 | nM | IC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum NF54 | F | 8.74 | pIC50 | 1.8 | nM | IC50 | Eur J Med Chem (2021) 210: 112955-112955 [PMID:33131885] |
| 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 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] |
| 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 | Antiplasmodial activity against asexual blood stage Plasmodium falciparum 3D7 infected in human RBC assessed as parasite growth inhibition incubated for 72 hrs by SYBR Green dye based fluorescence assay | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2021) 64: 2739-2761 [PMID:33620219] |
| 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 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 35:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
