PF-04856264 [Ligand Id: 14015] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2324000 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Nav1.7 in Human [GtoPdb: 584] [UniProtKB: Q15858] | ||||||||
| GtoPdb | - | - | 7.55 | pIC50 | 28 | nM | IC50 | Proc Natl Acad Sci U S A (2013) 110: E2724-32 [PMID:23818614] |
| Nav1.7/Sodium channel protein type 9 subunit alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414411] [GtoPdb: 584] [UniProtKB: Q62205] | ||||||||
| ChEMBL | Inhibition of mouse NaV1.7 by whole cell voltage clamp method | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
| 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 expressed in HEK293 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp method | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
| ChEMBL | Inhibition of NaV1.7 ion channel (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 261-263 [PMID:23177785] |
| GtoPdb | - | - | 7.55 | pIC50 | 28 | nM | IC50 | Proc Natl Acad Sci U S A (2013) 110: E2724-32 [PMID:23818614] |
| ChEMBL | Inhibition of human Nav1.7 | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4397-4401 [PMID:25176194] |
| ChEMBL | Inhibition of human NaV1.7 channel expressed in HEK293 cells by patch clamp electrophysiology assay | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2015) 58: 7093-7118 [PMID:25927480] |
| ChEMBL | Inhibition of human Nav1.7 expressed in HEK293 cells at -120 mV holding potential measured for 8 sec by patch-clamp method | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2087-2093 [PMID:28389149] |
| ChEMBL | Inhibition of human NaV1.7 | B | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
| 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 by cell based whole cell voltage clamp method | B | 5.38 | pIC50 | 4200 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
| 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 HEK295 cells at holding potential of -125 mV with test potentials to -10 mV by whole cell voltage clamp method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
| ChEMBL | Inhibition of human Nav1.5 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4397-4401 [PMID:25176194] |
| ChEMBL | Inhibition of human NaV1.5 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3477-3485 [PMID:28629594] |
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]
