lacosamide [Ligand Id: 7472] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL58323 (ADD 243037, ADD-243037, Erlosamide, Lacosamide, Lacosamide cv, (r)-lacosamide 1, SPM 927, SPM-927, 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 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]
