PF-05089771 [Ligand Id: 10723] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2325014 (Pf-05089771) |
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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 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414411] [GtoPdb: 584] [UniProtKB: Q62205] | ||||||||
| ChEMBL | Inhibition of mouse Nav1.7 in inactivated condition by automated patch-clamp assay | B | 8.1 | pIC50 | 8 | nM | IC50 | RSC Med Chem (2022) 13: 895-920 [PMID:36092147] |
| 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 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]
