DSM502 [Ligand Id: 11219] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4633246
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium vivax [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase/Dihydroorotate dehydrogenase (quinone), mitochondrial in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL3588732] [GtoPdb: 2949] [UniProtKB: Q08210]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum Dd2 [GtoPdb: 2949]
Created with Highcharts 10.3.3ValuesChart context menuPlasmodium falciparum dihydroorotate dehydrogenasepKd Plasmodium falciparumpKd Plasmodium falci…pKi Plasmodium falciparumpIC50 Plasmodium falciparumpEC50 Plasmodium falciparumpKd Plasmodium vivaxpKi Plasmodium vivaxpIC50 Plasmodium vivaxpEC50 Plasmodium vivaxpKd Plasmodium falciparum 3D7pKi Plasmodium falciparum 3D7pIC50 Plasmodium falciparum 3D7pEC50 Plasmodium falciparum 3D7pKd Plasmodium falciparum Dd2pKi Plasmodium falciparum Dd2pIC50 Plasmodium falciparum Dd2pEC50 Plasmodium falciparum Dd20246810Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuHERGpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuPlasmodium falciparumpKd Plasmodium falciparumpKi Plasmodium falciparumpIC50 Plasmodium falciparumpEC50 Plasmodium falciparum0246810Highcharts.com
  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
Created with Highcharts 10.3.3ValuesChart context menuVoltage-gated potassium channel subunit Kv1.5pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum [GtoPdb: 2949]
GtoPdb Steady-state kinetic analysis. - 7.7 pIC50 20 nM IC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium vivax [GtoPdb: 2949]
GtoPdb Steady-state kinetic analysis. - 7.85 pIC50 14 nM IC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Plasmodium falciparum dihydroorotate dehydrogenase/Dihydroorotate dehydrogenase (quinone), mitochondrial in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3588732] [GtoPdb: 2949] [UniProtKB: Q08210]
ChEMBL Inhibition of Plasmodium falciparum DHODH B 7.7 pIC50 20 nM IC50 J Med Chem (2023) 66: 8382-8406 [PMID:37357390]
GtoPdb Parasite growth inhibition assay - 7.85 pEC50 14 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum Dd2 [GtoPdb: 2949]
GtoPdb Parasite growth inhibition assay - 7.8 pEC50 16 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG by IonWorks patch clamp electrophysiology assay B 4.48 pEC50 >33000 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum R1AC1B harboring DHODH C276F mutant measured after 72 hrs by SYBR Green dye based fluorescence assay F 7.05 pEC50 89 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
ChEMBL Antimalarial activity against Plasmodium falciparum 1D3 measured after 72 hrs by SYBR Green dye based fluorescence assay F 7.08 pEC50 83 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 7.11 pEC50 78 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 7.62 pEC50 24 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 7.8 pEC50 16 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 7.8 pEC50 16 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 F 7.85 pEC50 14 nM EC50 J Med Chem (2023) 66: 8382-8406 [PMID:37357390]
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 7.85 pEC50 14 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
ChEMBL Antimalarial activity against drug-resistant Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in parasite growth measured after 72 hrs by SYBR Green method F 7.85 pEC50 14 nM EC50 J Med Chem (2021) 64: 6085-6136 [PMID:33876936]
ChEMBL Antimalarial activity against Plasmodium falciparum R1BC1A harboring DHODH L531F mutant measured after 72 hrs by SYBR Green dye based fluorescence assay F 7.89 pEC50 13 nM EC50 J Med Chem (2020) 63: 4929-4956 [PMID:32248693]
Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
ChEMBL Inhibition of human Kv1.5 by IonWorks patch clamp electrophysiology assay B 4.96 pEC50 >11000 nM EC50 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]