lamotrigine [Ligand Id: 2622] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL741 (BW 430C, BW-430C, Lamictal, Lamictal cd, Lamictal odt, Lamictal xr, Lamotrigine, NSC-759171)
  • Dihydrofolate reductase in Escherichia coli [ChEMBL: CHEMBL1809] [UniProtKB: P0ABQ4]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
  • Nav1.2/Sodium channel protein type II alpha subunit in Rat [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
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  • Nav1.3/Sodium channel protein type III alpha subunit in Human [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
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  • Nav1.4/Sodium channel protein type IV alpha subunit in Human [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
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  • Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Nav1.8/Sodium channel protein type X alpha subunit in Human [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
  • Nav1.8/Sodium channel protein type X alpha subunit in Rat [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Dihydrofolate reductase in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1809] [UniProtKB: P0ABQ4]
ChEMBL Inhibition of Escherichia coli DHFR assessed as NADP formation by quadratic Morrison plot analysis B 4.82 pKi 15240 nM Ki Eur. J. Med. Chem. (2015) 103: 600-614 [PMID:26414808]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Inhibition of [3H]pentazocine binding to Opioid receptor sigma 1 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (1999) 9: 2521-2524 [PMID:10498200]
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
ChEMBL Inhibition of human Nav1.2 channel expressed in HEK cells by patch-clamp electrophysiology method B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. (2009) 17: 3642-3648 [PMID:19394229]
ChEMBL Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay B 4.77 pIC50 17000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 650-654 [PMID:26101568]
ChEMBL Inhibition of human recombinant Nav1.2 channel expressed in HEK293 cells by whole cell voltage clamp technique B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. (2008) 16: 6379-6386 [PMID:18501613]
Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
ChEMBL Inhibition of rat Nav1.2 channel expressed in chinese hamster CHL1610 cells at preconditioning pulse of -67 mV after 2 to 3 mins by whole-cell patch-clamp technique B 4.46 pIC50 35000 nM IC50 J. Med. Chem. (2009) 52: 7528-7536 [PMID:19388676]
ChEMBL Inhibition of rat Nav1.2 expressed in CHL1610 cells at -67 to -107 mV after 2 to 3 mins by whole-cell patch-clamp assay B 4.46 pIC50 35000 nM IC50 J. Med. Chem. (2013) 56: 9019-9030 [PMID:24205976]
GtoPdb - - 4.5 pIC50 - - - Neuropharmacology (2003) 44: 413-22 [PMID:12604088];
Pflugers Arch (1995) 430: 437-46 [PMID:7491269]
Nav1.3/Sodium channel protein type III alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
ChEMBL Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay B 4.77 pIC50 17000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 650-654 [PMID:26101568]
Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
ChEMBL Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells B 4.77 pKi 17000 nM Ki J. Med. Chem. (2004) 47: 1547-1552 [PMID:14998340]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay B 4.77 pIC50 17000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 650-654 [PMID:26101568]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 4 pIC50 100000 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of human recombinant Nav1.5 channel expressed in HEK293 cells by whole cell voltage clamp technique B 4.21 pIC50 62000 nM IC50 Bioorg. Med. Chem. (2008) 16: 6379-6386 [PMID:18501613]
ChEMBL Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform F 4.4 pIC50 39810.72 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
Nav1.8/Sodium channel protein type X alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
ChEMBL Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay B 4.01 pIC50 98000 nM IC50 ACS Med. Chem. Lett. (2015) 6: 650-654 [PMID:26101568]
ChEMBL Inhibition of human recombinant Nav1.8 channel expressed in HEK293 cells by whole cell voltage clamp technique B 4.02 pIC50 96000 nM IC50 Bioorg. Med. Chem. (2008) 16: 6379-6386 [PMID:18501613]
Nav1.8/Sodium channel protein type X alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968]
ChEMBL Blockade of Nav1.8 channel in rat dorsal root ganglion neurons assessed as inhibition of TTX-R current by whole cell patch clamp technique B 4.6 pIC50 25000 nM IC50 Bioorg. Med. Chem. (2008) 16: 6379-6386 [PMID:18501613]

ChEMBL data shown on this page come from version 28:

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]