riluzole [Ligand Id: 2326] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL744 (BHV-0223, Exservan, NSC-753433, NSC-759823, Rilutek, Riluzole, RP 54274, RP-54274, Teglutik, Tiglutik, Tiglutik kit) |
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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] | ||||||||
| GtoPdb | Inhibition of currents via human Kv11.1 (hERG) channels expressed in HEK293 cells in whole-cell patch-clamp experiments. | - | 4.3 | pIC50 | 50000 | nM | IC50 | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| ChEMBL | Displacement of Tracer Red from human ERG by fluorescence polarization assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | J Med Chem (2019) 62: 3989-4012 [PMID:30908048] |
| 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 | 5.76 | pKi | 1718 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.76 | pIC50 | 1733 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Pteridine reductase 1 in Leishmania major (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6194] [UniProtKB: Q01782] | ||||||||
| ChEMBL | Inhibition of Leishmania major PTR1 by Lineweaver-Burk analysis | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2011) 54: 211-221 [PMID:21126022] |
| ChEMBL | Inhibition of Leishmania major pteridine reductase 1 using di-hydrobiopterine as substrate in presence of NADPH | B | 4.03 | pIC50 | 94100 | nM | IC50 | J Med Chem (2019) 62: 3989-4012 [PMID:30908048] |
| ChEMBL | Inhibition of Leishmania major PTR1 | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2011) 54: 211-221 [PMID:21126022] |
| Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250] | ||||||||
| ChEMBL | Blockade of synaptosomal sodium channels, inhibition of [14C]guanidinium ion flux into CHO cells expressing Type II sodium channel | F | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 2259-2262 |
| Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775] | ||||||||
| ChEMBL | Sodium channel block, determined by % block of [14C]guanidinium flux in CHO line expressing rat type IIA sodium channels derived from rat brain | F | 5.33 | pIC50 | 4730 | nM | IC50 | J Med Chem (1998) 41: 3298-3302 [PMID:9703475] |
| KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952] | ||||||||
| GtoPdb | - | - | 4.68 | pEC50 | 21000 | nM | EC50 | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604] | ||||||||
| GtoPdb | - | - | 4.89 | pEC50 | 12800 | nM | EC50 | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| KCa2.3 in Human [GtoPdb: 383] [UniProtKB: Q9UGI6] | ||||||||
| GtoPdb | - | - | 4.9 | pEC50 | 12500 | nM | EC50 | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554] | ||||||||
| GtoPdb | - | - | 5.7 | pIC50 | - | - | - | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 5.04 | pEC50 | 9200 | nM | EC50 | Br J Pharmacol (2014) 171: 158-70 [PMID:24117252] |
| Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881] | ||||||||
| GtoPdb | Inhibition of currents via rat Kv4.2 channels expressed in LTK cells in whole-cell patch-clamp experiments. | - | 3.89 | pIC50 | 130000 | nM | IC50 | Mol Pharmacol (2009) 75: 281-95 [PMID:18955585] |
| Kv4.3 in Rat [GtoPdb: 554] [UniProtKB: Q62897] | ||||||||
| GtoPdb | - | - | 3.9 | pIC50 | - | - | - | J Pharmacol Exp Ther (2006) 319: 323-31 [PMID:16815868] |
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]
