ranolazine [Ligand Id: 7291] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1404 (Aspruzyo, Aspruzyo sprinkle, CVT-303, NSC-759100, Ran d, Ranexa, Ranolazine, RS-43285-003) |
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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 human ERG expressed in CHO cells using voltage step to -50 mV for 300 ms from -80 mV holding potential by automated patch clamp assay | B | 4.87 | pIC50 | 13400 | nM | IC50 | US-8586732-B2. Fused heterocyclic compounds as ion channel modulators (2013) |
| ChEMBL | Inhibition of human ERG expressed stably in CHO cells by manual patch clamp technique | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2016) 59: 9005-9017 [PMID:27690427] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of Nav1.5 (unknown origin)-mediated late channel current | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2021) 45: 128133-128133 [PMID:34044121] |
| ChEMBL | Inhibition of human NaV1.5 expressed in HEK293 cells assessed as blocking of tefluthrin-induced late sodium currents using -20 mV voltage steps at holding potential of -120 mV by whole cell patch clamp Qpatch method | B | 5.17 | pIC50 | 6700 | nM | IC50 | US-8586732-B2. Fused heterocyclic compounds as ion channel modulators (2013) |
| Voltage-gated sodium channel Nav1.5 cardiac isoform in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3808271] [UniProtKB: Q5YLN7] | ||||||||
| ChEMBL | Inhibition of canine ventricular myocytes Nav 1.5 assessed as reduction in ATX-2 induced late channel current by manual single-patch clamp assay | B | 5.16 | pIC50 | 6900 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3202-3206 [PMID:27080178] |
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]
