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) |
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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 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]
