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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 |
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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]