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, Ranexa (previously latixa), Ranolazina, 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 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]
