| Reaction Details |
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 | Report a problem with these data |
| Target | Voltage-gated sodium channel Nav1.5 cardiac isoform |
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| Ligand | BDBM50173335 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1580046 (CHEMBL3810731) |
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| IC50 | 6900±n/a nM |
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| Citation |  Koltun, DO; Parkhill, EQ; Elzein, E; Kobayashi, T; Notte, GT; Kalla, R; Jiang, RH; Li, X; Perry, TD; Avila, B; Wang, WQ; Smith-Maxwell, C; Dhalla, AK; Rajamani, S; Stafford, B; Tang, J; Mollova, N; Belardinelli, L; Zablocki, JA Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine. Bioorg Med Chem Lett26:3202-6 (2016) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Voltage-gated sodium channel Nav1.5 cardiac isoform |
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| Name: | Voltage-gated sodium channel Nav1.5 cardiac isoform |
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| Synonyms: | SCN5A | Voltage-gated sodium channel Nav1.5 cardiac isoform |
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| Type: | PROTEIN |
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| Mol. Mass.: | 16812.22 |
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| Organism: | Canis lupus familiaris |
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| Description: | ChEMBL_116798 |
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| Residue: | 159 |
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| Sequence: | GLLQRPPKPTALAAHGQLPGCMATSSSPPPPESQKVPPARKETRFEEDKQPGQGTPGDTE
PVCVPIAMAESDTDDQEEDEENSLGTEEESSKQQESQPVSGSPEAVPERGAWSQVSETAS
SEASVAQADWRQQRKVEPPAPGCSEAPEDSYSEGSTADM
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| BDBM50173335 |
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| n/a |
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| Name | BDBM50173335 |
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| Synonyms: | CHEBI:87690 | CVT-303 | RS-43285-003 | Ranexa | Ranolazine |
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| Type | Small organic molecule |
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| Emp. Form. | C24H33N3O4 |
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| Mol. Mass. | 427.5365 |
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| SMILES | COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 |
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| Structure | 
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