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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL960 (Leflunomide, HWA-486, L04AA13, SU-101, SULOL, Arava, SU101)
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
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]
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 28:

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]