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 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]