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, SU-101, SU101, SULOL) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
