lacosamide [Ligand Id: 7472] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL58323 (ADD 243037, ADD-243037, ADD243037, Erlosamide, Lacosamida, Lacosamide, Lacosamide cv, Motpoly, (r)-lacosamide 1, SPM 927, SPM-927, SPM927, Vimpat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23] | ||||||||
| ChEMBL | Inhibition of mouse recombinant CA15 by stopped flow CO2 hydrase assay | B | 6.34 | pKi | 461 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of human recombinant CA1 by stopped flow CO2 hydrase assay | B | 6.44 | pKi | 362 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of human recombinant CA2 by stopped flow CO2 hydrase assay | B | 6.48 | pKi | 331 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| Carbonic anhydrase III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2885] [UniProtKB: P07451] | ||||||||
| ChEMBL | Inhibition of human recombinant CA3 by stopped flow CO2 hydrase assay | B | 6.43 | pKi | 374 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human recombinant CA4 by stopped flow CO2 hydrase assay | B | 6.28 | pKi | 525 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of human recombinant CA9 by stopped flow CO2 hydrase assay | B | 6.45 | pKi | 353 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of human recombinant CA5A by stopped flow CO2 hydrase assay | B | 5.34 | pKi | 4565 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of human recombinant CA5B by stopped flow CO2 hydrase assay | B | 6.47 | pKi | 341 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of human recombinant CA6 by stopped flow CO2 hydrase assay | B | 6.39 | pKi | 412 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| ChEMBL | Inhibition of human recombinant CA7 by stopped flow CO2 hydrase assay | B | 5.35 | pKi | 4446 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of human recombinant CA12 by stopped flow CO2 hydrase assay | B | 5.43 | pKi | 3713 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1] | ||||||||
| ChEMBL | Inhibition of human recombinant CA13 by stopped flow CO2 hydrase assay | B | 5.92 | pKi | 1210 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7] | ||||||||
| ChEMBL | Inhibition of human recombinant CA14 by stopped flow CO2 hydrase assay | B | 6.33 | pKi | 473 | nM | Ki | J Med Chem (2010) 53: 850-854 [PMID:20028100] |
| Nav1.3/Sodium channel protein type III alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4966] [GtoPdb: 580] [UniProtKB: P08104] | ||||||||
| GtoPdb | - | - | 3.4 | pIC50 | 415000 | nM | IC50 | J Pharmacol Exp Ther (2008) 326: 89-99 [PMID:18378801] |
| ChEMBL | Binding affinity to rat inactivated voltage-gated Na channel 1.3 expressed in human HEK293 cells by patch-clamp technique | B | 6.38 | pIC50 | 415 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| ChEMBL | Inhibition of rat NaV1.3 expressed in HEK293 cells at -80V holding potential by whole-cell patch-Clamp method | B | 6.38 | pIC50 | 415 | nM | IC50 | Medchemcomm (2017) 8: 1255-1267 [PMID:30108836] |
| Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858] | ||||||||
| GtoPdb | - | - | 3.7 | pIC50 | 182000 | nM | IC50 | J Pharmacol Exp Ther (2008) 326: 89-99 [PMID:18378801] |
| ChEMBL | Binding affinity to human inactivated voltage-gated Na channel 1.7 expressed in HEK293 cells by patch-clamp technique | B | 6.74 | pIC50 | 182 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| Nav1.8/Sodium channel protein type X alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968] | ||||||||
| ChEMBL | Binding affinity to voltage-gated Na channel 1.8 in Sprague-Dawley rat L4/L5 DRG neurons by patch-clamp technique | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2013) 56: 593-624 [PMID:23121096] |
| GtoPdb | - | - | 4.8 | pIC50 | 16000 | nM | IC50 | J Pharmacol Exp Ther (2008) 326: 89-99 [PMID:18378801] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform | F | 4.3 | pIC50 | 50118.72 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775] | ||||||||
| GtoPdb | - | - | 4.52 | pIC50 | 30000 | nM | IC50 | Front Pharmacol (2013) 4: 121 [PMID:24065921] |
ChEMBL data shown on this page come from version 34:
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]
