lacosamide [Ligand Id: 7472] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL58323 (Vimpat, ADD-243037, SPM-927, Lacosamide, Erlosamide)
  • Carbonic anhydrase 15 in Mouse [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23]
  • This target only has 1 pki data point
1 CHEMBL58323_lig_chart_1 Carbonic anhydrase 15 Mouse
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
  • This target only has 1 pki data point
2 CHEMBL58323_lig_chart_2 Carbonic anhydrase I Human
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
  • This target only has 1 pki data point
3 CHEMBL58323_lig_chart_3 Carbonic anhydrase II Human
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  • Carbonic anhydrase III in Human [ChEMBL: CHEMBL2885] [UniProtKB: P07451]
  • This target only has 1 pki data point
4 CHEMBL58323_lig_chart_4 Carbonic anhydrase III Human
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  • carbonic anhydrase 4/Carbonic anhydrase IV in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
  • This target only has 1 pki data point
5 CHEMBL58323_lig_chart_5 Carbonic anhydrase IV Human
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
  • This target only has 1 pki data point
6 CHEMBL58323_lig_chart_6 Carbonic anhydrase IX Human
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  • carbonic anhydrase 5A/Carbonic anhydrase VA in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
  • This target only has 1 pki data point
7 CHEMBL58323_lig_chart_7 Carbonic anhydrase VA Human
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  • Carbonic anhydrase VB in Human [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
  • This target only has 1 pki data point
8 CHEMBL58323_lig_chart_8 Carbonic anhydrase VB Human
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  • Carbonic anhydrase VI in Human [ChEMBL: CHEMBL3025] [UniProtKB: P23280]
  • This target only has 1 pki data point
9 CHEMBL58323_lig_chart_9 Carbonic anhydrase VI Human
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  • carbonic anhydrase 7/Carbonic anhydrase VII in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
  • This target only has 1 pki data point
10 CHEMBL58323_lig_chart_10 Carbonic anhydrase VII Human
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
  • This target only has 1 pki data point
11 CHEMBL58323_lig_chart_11 Carbonic anhydrase XII Human
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  • carbonic anhydrase 13/Carbonic anhydrase XIII in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
  • This target only has 1 pki data point
12 CHEMBL58323_lig_chart_12 Carbonic anhydrase XIII Human
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  • carbonic anhydrase 14/Carbonic anhydrase XIV in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
  • This target only has 1 pki data point
13 CHEMBL58323_lig_chart_13 Carbonic anhydrase XIV Human
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  • Nav1.3/Sodium channel protein type III alpha subunit in Rat [ChEMBL: CHEMBL4966] [GtoPdb: 580] [UniProtKB: P08104]
  • This target only has 0 pki data point
14 CHEMBL58323_lig_chart_14 Sodium channel protein type III alpha subunit Rat
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  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
  • This target only has 0 pki data point
15 CHEMBL58323_lig_chart_15 Sodium channel protein type IX alpha subunit Human
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  • Nav1.8/Sodium channel protein type X alpha subunit in Rat [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
  • This target only has 0 pki data point
16 CHEMBL58323_lig_chart_16 Sodium channel protein type X alpha subunit Rat
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • This target only has 0 pki data point
17 CHEMBL58323_lig_chart_17 Voltage-gated L-type calcium channel alpha-1C subunit Human
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  • Nav1.2 in Rat [GtoPdb: 579] [UniProtKB: P04775]
  • This target only has 0 pki data point
18 CHEMBL58323_lig_chart_18 Nav1.2 Rat
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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
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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]