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ChEMBL ligand: CHEMBL3707218 (Funapide, Tv-45070, TV-45070, XEN-401-S, XEN-402, XEN402, XPF-002) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]