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) |
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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 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 (null) |
| 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 (null) |
| 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] |
| 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 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
