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

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ChEMBL ligand: CHEMBL4633246
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  • Kv1.5/Voltage-gated potassium channel subunit Kv1.5 in Human [ChEMBL: CHEMBL4306] [GtoPdb: 542] [UniProtKB: P22460]
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  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium vivax [GtoPdb: 2949]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum 3D7 [GtoPdb: 2949] [UniProtKB: Q08210]
  • Plasmodium falciparum dihydroorotate dehydrogenase in Plasmodium falciparum Dd2 [GtoPdb: 2949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]
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 in Plasmodium falciparum 3D7 [GtoPdb: 2949] [UniProtKB: Q08210]
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]

ChEMBL data shown on this page come from version 31:

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]