PF-05089771 [Ligand Id: 10723] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2325014 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Nav1.7/Sodium channel protein type 9 subunit alpha/beta-1/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4630765] [GtoPdb: 584] [UniProtKB: O60939, Q07699, Q15858] | ||||||||
| ChEMBL | Inhibition of human NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2020) 63: 10204-10220 [PMID:32392056] |
| Nav1.7/Sodium channel protein type 9 subunit alpha/beta-1/beta-2 in Mouse (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4630766] [GtoPdb: 584] [UniProtKB: P97952, Q56A07, Q62205] | ||||||||
| ChEMBL | Inhibition of mouse NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2020) 63: 10204-10220 [PMID:32392056] |
| 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 expressed in HEK293 cells by electrophysiology assay | B | 6.07 | pIC50 | 850 | nM | IC50 | J Med Chem (2019) 62: 8695-8710 [PMID:31012583] |
| 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 expressed in HEK293 cells by electrophysiology assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2019) 62: 8695-8710 [PMID:31012583] |
| 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 Nav1.3 expressed in HEK293 cells by electrophysiology assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2019) 62: 8695-8710 [PMID:31012583] |
| ChEMBL | Inhibition of human NaV1.3 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 7029-7042 [PMID:28682065] |
| 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 expressed in HEK293 cells by electrophysiology assay | B | 5 | pIC50 | 10000 | 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 | Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2683-2688 [PMID:28465103] |
| ChEMBL | Inhibition of human Nav1.7 expressed in CHO-K1 cells at -120 mV holding potential incubated over 5 mins measured at 15 secs interval by Qpatch clamp assay | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2210-2215 [PMID:28385504] |
| ChEMBL | Inhibition of human Nav1.7 expressed in HEK293 cells | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2087-2093 [PMID:28389149] |
| ChEMBL | Inhibition of human NaV1.7 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2017) 60: 7029-7042 [PMID:28682065] |
| ChEMBL | Inhibition of recombinant human Nav1.7 expressed in HEK293 cells by voltage clamp electrophysiology method | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4805-4811 [PMID:29029933] |
| ChEMBL | Inhibition of NaV1.7 ion channel (unknown origin) | B | 8.07 | pIC50 | 8.6 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 261-263 [PMID:23177785] |
| 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 expressed in HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method | B | 6.82 | pIC50 | 153 | nM | IC50 | J Med Chem (2017) 60: 7029-7042 [PMID:28682065] |
| 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 | 4.6 | pIC50 | 25000 | 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 | 7.96 | pIC50 | 11 | 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 | 6.8 | pIC50 | 160 | 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 HEK cells assessed as half inactivation potential at -120 mV holding potential by automated patch clamp method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 7029-7042 [PMID:28682065] |
| ChEMBL | Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2019) 62: 8695-8710 [PMID:31012583] |
| Urate anion exchanger 1/Solute carrier family 22 member 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37] | ||||||||
| ChEMBL | Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting | B | 5.46 | pIC50 | 3500 | nM | IC50 | Medchemcomm (2016) 7: 1587-1595 |
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]
