ICA-121431 [Ligand Id: 14012] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3617053
  • Nav1.1/Sodium channel protein type I alpha subunit in Human [ChEMBL: CHEMBL1845] [GtoPdb: 578] [UniProtKB: P35498]
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  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
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  • Nav1.3/Sodium channel protein type III alpha subunit in Human [ChEMBL: CHEMBL5163] [GtoPdb: 580] [UniProtKB: Q9NY46]
  • Nav1.3/Sodium channel protein type III alpha subunit in Rat [ChEMBL: CHEMBL4966] [GtoPdb: 580] [UniProtKB: P08104]
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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]
  • Nav1.7/Sodium channel protein type IX alpha subunit in Rat [ChEMBL: CHEMBL3312] [GtoPdb: 584] [UniProtKB: O08562]
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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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  • Nav1.6/Sodium channel protein type VIII alpha subunit in Human [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0]
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  • Nav1.8/Sodium channel protein type X alpha subunit in Human [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Nav1.1/Sodium channel protein type I alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1845] [GtoPdb: 578] [UniProtKB: P35498]
ChEMBL Inhibition of human NaV1.1 B 7.49 pIC50 32 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
ChEMBL Inhibition of human NaV1.1 channel by patch clamp electrophysiology assay B 7.7 pIC50 <20 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
GtoPdb - - 7.72 pIC50 19 nM IC50 Proc Natl Acad Sci U S A (2013) 110: E2724-32 [PMID:23818614]
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 B 6.41 pIC50 393 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
ChEMBL Inhibition of human NaV1.2 channel by patch clamp electrophysiology assay B 6.62 pIC50 240 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
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 TTX-sensitive NaV1.3 channel expressed in HEK293 cells by patch clamp electrophysiology assay B 7.7 pIC50 <20 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
GtoPdb - - 7.72 pIC50 19 nM IC50 Proc Natl Acad Sci U S A (2013) 110: E2724-32 [PMID:23818614]
ChEMBL Inhibition of human NaV1.3 expressed in HEK cells by electrophysiological method B 7.77 pIC50 17 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
Nav1.3/Sodium channel protein type III alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4966] [GtoPdb: 580] [UniProtKB: P08104]
ChEMBL Inhibition of rat NaV1.3 by electrophysiological method B 8.22 pIC50 6 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
ChEMBL Inhibition of human NaV1.4 channel by patch clamp electrophysiology assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
ChEMBL Inhibition of human NaV1.4 B 5 pIC50 10000 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
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 channel expressed in HEK293 cells by patch clamp electrophysiology assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
ChEMBL Inhibition of human NaV1.7 B 5.28 pIC50 5200 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
Nav1.7/Sodium channel protein type IX alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3312] [GtoPdb: 584] [UniProtKB: O08562]
ChEMBL Inhibition of rat NaV1.7 B 7.17 pIC50 68 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
ChEMBL Inhibition of human NaV1.5 channel expressed in HEK293 cells by patch clamp electrophysiology assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
ChEMBL Inhibition of human NaV1.5 B 5.04 pIC50 9200 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
Nav1.6/Sodium channel protein type VIII alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0]
ChEMBL Inhibition of human NaV1.6 B 4.99 pIC50 10300 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]
ChEMBL Inhibition of human NaV1.6 channel by patch clamp electrophysiology assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
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 channel by patch clamp electrophysiology assay B 5 pIC50 >10000 nM IC50 J Med Chem (2015) 58: 7093-7118 [PMID:25927480]
ChEMBL Inhibition of human NaV1.8 B 5.52 pIC50 3000 nM IC50 Medchemcomm (2017) 8: 1255-1267 [PMID:30108836]

ChEMBL data shown on this page come from version 35:

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]