funapide [Ligand Id: 12644] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3707218 (Funapide, Tv-45070, TV-45070, XEN-401-S, XEN-402, XEN402, XPF-002)
  • Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
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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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  • Sodium channel protein type VII alpha subunit in Human [ChEMBL: CHEMBL3585] [UniProtKB: Q01118]
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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
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
GtoPdb Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay - 6.22 pIC50 600 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
ChEMBL Inhibition of Nav1.2 (unknown origin) B 6.22 pIC50 601 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
ChEMBL Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay B 6.22 pIC50 600 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL Binding affinity to inactivated state of human Nav1.7 expressed in HEK293 cells by whole cell voltage clamp assay B 6.79 pKd 161 nM Kd US-8450358-B2. Enantiomers of spiro-oxindole compounds and their uses as therapeutic agents (2013)
ChEMBL Inhibition of human Nav1.7 B 7.27 pIC50 54 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
GtoPdb Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay - 7.27 pIC50 54 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
ChEMBL In Vitro Assay: The assay is based on the guanidine influx assay described by Reddy, N. L., et al., J. Med. Chem. (1998), 41(17):3298-302. The guanidine influx assay is a radiotracer flux assay used to determine ion flux activity of voltage-gated sodium channels in a high-throughput microplate-based format. The assay uses 14C-guanidine hydrochloride in combination with various known voltage-gated sodium channel modulators that produce maintained influx, to assay the potency of test agents. B 8.52 pIC50 3 nM IC50 US-9260446-B2. Synthetic methods for spiro-oxindole compounds (2016)
ChEMBL Inhibition of human Nav1.7 expressed in HEK293 cells assessed as reduction in 14C-guanidinium influx by scintillation counting analysis B 8.52 pIC50 3 nM IC50 US-8450358-B2. Enantiomers of spiro-oxindole compounds and their uses as therapeutic agents (2013)
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 expressed in HEK293 cells by electrophysiology assay B 7.08 pIC50 84 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
ChEMBL Inhibition of human Nav1.5 B 7.08 pIC50 84 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
GtoPdb Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay - 7.08 pIC50 84 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
Sodium channel protein type VII alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3585] [UniProtKB: Q01118]
ChEMBL Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay B 7.27 pIC50 54 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
Nav1.6/Sodium channel protein type VIII alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0]
ChEMBL Inhibition of Nav1.6 (unknown origin) B 6.76 pIC50 173 nM IC50 RSC Med Chem (2022) 13: 895-920 [PMID:36092147]
ChEMBL Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay B 6.77 pIC50 170 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
GtoPdb Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay - 6.77 pIC50 170 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
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 by electrophysiology assay B 5.32 pIC50 4800 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]
GtoPdb Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay - 5.32 pIC50 4800 nM IC50 J Med Chem (2019) 62: 8695-8710 [PMID:31012583]

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]