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 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]
