N-Me-aminopyrimidinone 9 [Ligand Id: 5733] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1938867
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of dofetilide from human ERG B 4.82 pKi >15000 nM Ki Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Antagonist activity at non-inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by manual patch-clamp electrophysiological assay F 6.3 pIC50 500 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]
ChEMBL Antagonist activity at 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay F 6.38 pIC50 420 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]
ChEMBL Antagonist activity at 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by manual patch-clamp electrophysiological assay F 7.1 pIC50 80 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]
GtoPdb Electrophysiology - 7.1 pIC50 80 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-60 [PMID:22209205]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Antagonist activity at partially inactivated human sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay F 6.7 pIC50 200 nM IC50 Bioorg Med Chem Lett (2012) 22: 1055-1060 [PMID:22209205]

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]