leflunomide [Ligand Id: 6825] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL960 (Arava, HWA-486, L04AA13, Leflunomide, Leflunomide medac, Leflunomide ratiopharm, Leflunomide teva, Leflunomide winthrop, NSC-677411, NSC-759864, Repso, SU101, SU-101, SULOL)
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  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Mouse [ChEMBL: CHEMBL2991] [GtoPdb: 2604] [UniProtKB: O35435]
  • dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Rat [ChEMBL: CHEMBL2383] [GtoPdb: 2604] [UniProtKB: Q63707]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 6.3 pIC50 500 nM IC50 DrugMatrix in vitro pharmacology data
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
GtoPdb - - 4.89 pKi 13000 nM Ki J Med Chem (1998) 41: 3530-8 [PMID:9719606]
ChEMBL In vitro inhibitory activity against human dihydroorotate dehydrogenase (DHODH) B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (1998) 41: 3530-3538 [PMID:9719606]
ChEMBL Immunosuppressive activity expressed as ability to inhibit human recombinant dihydroorotate dehydrogenase (DHODH) B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2203-2208 [PMID:9873513]
ChEMBL Inhibition of human DHODH B 6.1 pIC50 800 nM IC50 Bioorg Med Chem Lett (2021) 46: 128194-128194 [PMID:34116160]
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2991] [GtoPdb: 2604] [UniProtKB: O35435]
ChEMBL Inhibitory concentration tested on enzyme dihydroorotate dehydrogenase in mouse B 7.52 pIC50 30 nM IC50 J. Med. Chem. (1996) 39: 4608-4621 [PMID:8917650]
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2383] [GtoPdb: 2604] [UniProtKB: Q63707]
ChEMBL Inhibition of DHODH in Wistar rat liver homogenates by DCIP reduction assay B 5.8 pIC50 1600 nM IC50 Eur. J. Med. Chem. (2011) 46: 383-392 [PMID:21109332]
ChEMBL Inhibitory concentration tested against enzyme dihydroorotate dehydrogenase in rat B 8.05 pIC50 9 nM IC50 J. Med. Chem. (1996) 39: 4608-4621 [PMID:8917650]
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.64 pKi 2291 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.54 pIC50 2884 nM IC50 DrugMatrix in vitro pharmacology data
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) B 4.68 pIC50 20696 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.34 pKi 4591 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.33 pIC50 4630 nM IC50 DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 4.73 pIC50 >18500 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]