leflunomide [Ligand Id: 6825] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL960 (Arava, HWA-486, L04AA13, Leflunomida, Leflunomide, Leflunomide medac, Leflunomide ratiopharm, Leflunomide teva, Leflunomide winthrop, Leflunomide zentiva (previously 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 |
|---|---|---|---|---|---|---|---|---|
| Monoamine oxidase A/Amine oxidase [flavin-containing] 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 |
| 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 (quinone), mitochondrial 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 (quinone), mitochondrial 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 (quinone), mitochondrial 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] |
| 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 |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of C-terminal His-tagged human recombinant PIM-1 expressed in Escherichia coli BL21 (DE3) cells using RSRHSSYPAGT as peptide substrate preincubated for 15 mins followed by substrate addition measured after 1hr by Hot-SpotSM kinase assay | B | 4.54 | pIC50 | 28700 | nM | IC50 | Eur J Med Chem (2024) 264: 116016-116016 [PMID:38071792] |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of PIM-3 (unknown origin) | B | 4.69 | pIC50 | 20600 | nM | IC50 | Eur J Med Chem (2024) 264: 116016-116016 [PMID:38071792] |
| DAT/Sodium-dependent 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 |
| NET/Sodium-dependent noradrenaline 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 |
ChEMBL data shown on this page come from version 36:
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]
