PF-04885614 [Ligand Id: 11864] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4084106 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of recombinant human ERG expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method | B | 5.59 | pIC50 | 2600 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| GtoPdb | Inhibition of hERG measured in a fluorescence polarisation assay, using hERG expressed in HEK-293S cells. | - | 5.74 | pIC50 | 1800 | nM | IC50 | Med. Chem. Commun (2016) 7: 1925-1931 |
| ChEMBL | Inhibition of Cy3B-labeled ligand binding to recombinant human ERG expressed in HEK293 cells by fluorescence polarization method | B | 5.74 | pIC50 | 1800 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| Nav1.1/Sodium channel protein type I alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1845] [GtoPdb: 578] [UniProtKB: P35498] | ||||||||
| ChEMBL | Inhibition of 50% inactivated recombinant human Nav1.1 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method | B | 4.96 | pIC50 | 11000 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250] | ||||||||
| ChEMBL | Inhibition of 50% inactivated recombinant human Nav1.2 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method | B | 4.8 | pIC50 | 16000 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| 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 recombinant human Nav1.7 expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method | B | 5.15 | pIC50 | 7000 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| Nav1.6/Sodium channel protein type VIII alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5202] [GtoPdb: 583] [UniProtKB: Q9UQD0] | ||||||||
| ChEMBL | Inhibition of 50% inactivated recombinant human Nav1.6 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method | B | 5.38 | pIC50 | 4200 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| GtoPdb | - | - | 5.38 | pIC50 | 4200 | nM | IC50 | Med. Chem. Commun (2016) 7: 1925-1931 |
| Nav1.8/Sodium channel protein type X alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5451] [GtoPdb: 585] [UniProtKB: Q9Y5Y9] | ||||||||
| ChEMBL | Inhibition of 50% inactivated recombinant human Nav1.8 expressed in HEK293 cells coexpressing Nav beta1 subunit at holding potential of -120 mV by manual patch electrophysiology method | B | 7.28 | pIC50 | 53 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
| GtoPdb | - | - | 7.28 | pIC50 | 53 | nM | IC50 | Med. Chem. Commun (2016) 7: 1925-1931 |
| Nav1.8/Sodium channel protein type X alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4017] [GtoPdb: 585] [UniProtKB: Q62968] | ||||||||
| ChEMBL | Inhibition of Nav1.8 in rat DRG neurons assessed as inhibition of TTX-resistant current at holding potential of -120 mV by manual patch electrophysiology method | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2016) 7: 1925-1931 |
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]
