| Assay ID | Title | Year | Journal | Article |
|---|
| AID1302457 | Volume of distribution at steady state in iv dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302469 | Inhibition of human Nav 1.5 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302478 | Inhibition of human Nav 1.6 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302489 | Inhibition of human Nav 1.1 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302459 | Clearance in iv dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302467 | Inhibition of human Nav 1.3 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302107 | Ratio of drug level in brain to plasma in rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302486 | Inhibition of human Nav 1.6 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302496 | Inhibition of human Nav 1.8 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302495 | Inhibition of human Nav 1.7 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302075 | Inhibition of 3 Hz stimulated Nav1.5 (unknown origin) assessed as inhibition of peak sodium current by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302476 | Inhibition of human Nav 1.4 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302437 | Inhibition of Nav 1.5 (unknown origin) assessed as reduction in peak channel current at 0.1 uM measured at 3 Hz | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302448 | Permeability from basolateral to apical side in human Caco2 cells at 1 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302490 | Inhibition of human Nav 1.2 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302447 | Permeability from apical to basolateral side in human Caco2 cells at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302440 | Lipophilicity, logD of the compound | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302080 | Inhibition of 10 Hz stimulated Nav1.2 (unknown origin) by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302079 | Inhibition of 1 Hz stimulated Nav1.2 (unknown origin) by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302477 | Inhibition of human Nav 1.5 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302434 | Inhibition of Nav 1.5 (unknown origin) assessed as reduction in peak channel current at 0.1 uM measured at 1 Hz | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302492 | Inhibition of human Nav 1.4 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302456 | Volume of distribution at steady state in iv dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302462 | Oral bioavailability in rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302063 | Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluthrin/ATX2 m | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302073 | Inhibition of Nav1.5 (unknown origin) assessed as inhibition of late sodium current by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302464 | Inhibition of human ERG at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302449 | Permeability from basolateral to apical side in human Caco2 cells at 10 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302454 | Tmax in po dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302445 | Stability in dog liver microsomes | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302076 | Inhibition of 1 Hz stimulated Nav1.1 (unknown origin) by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302466 | Inhibition of human Nav 1.2 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302479 | Inhibition of human Nav 1.7 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302450 | AUC (0 to infinity) in po dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302458 | Clearance in iv dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302061 | Inhibition of 0.1 Hz stimulated human Nav1.5alpha expressed in HEK293 cells assessed as inhibition of late sodium current at 0.1 uM with 3 compound additions for 7 to 8 mins at holding potential -120 mV in presence of late sodium current activator tefluth | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302497 | Inhibition of Nav 1.5 in langerdorff isolated heart model (unknown origin) assessed as reversal of ATX-2 induced increase in monophasic action potential duration | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302451 | AUC (0 to infinity) in po dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302481 | Inhibition of human Nav 1.1 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302483 | Inhibition of human Nav 1.3 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302452 | Cmax in po dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302480 | Inhibition of human Nav 1.8 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302443 | Stability in human liver microsomes | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302074 | Inhibition of 1 Hz stimulated Nav1.5 (unknown origin) assessed as inhibition of peak sodium current by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302077 | Inhibition of 10 Hz stimulated Nav1.1 (unknown origin) by manual patch clamp method | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302460 | Tmax in iv dosed rat | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302493 | Inhibition of human Nav 1.5 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302487 | Inhibition of human Nav 1.7 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302482 | Inhibition of human Nav 1.2 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302446 | Permeability from apical to basolateral side in human Caco2 cells at 1 uM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302463 | Oral bioavailability in cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302474 | Inhibition of human Nav 1.2 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302471 | Inhibition of human Nav 1.7 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302498 | Protection from methoxamine/clofilium induced ventricular arrhythmias in anesthetized rabbit assessed as decrease in torsade des pointes at 300 nM | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302472 | Inhibition of human Nav 1.8 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302491 | Inhibition of human Nav 1.3 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302108 | Ratio of drug level in brain to plasma in dog | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302461 | Tmax in iv dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302442 | Aqueous solubility of the compound in PBS at pH 7.6 | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302473 | Inhibition of human Nav 1.1 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302465 | Inhibition of human Nav 1.1 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302078 | Inhibition of human ERG | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine. |
| AID1302470 | Inhibition of human Nav 1.6 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302441 | Aqueous solubility of the compound in HCL at pH 2.2 | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302444 | Stability in rat liver microsomes | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302468 | Inhibition of human Nav 1.4 assessed as reduction in peak channel current at 1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302488 | Inhibition of human Nav 1.8 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302484 | Inhibition of human Nav 1.4 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302455 | Tmax in po dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302475 | Inhibition of human Nav 1.3 assessed as reduction in peak channel current at 0.1 uM measured at 0.1 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302433 | Inhibition of Nav 1.5 (unknown origin) assessed as reduction in late channel current | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302485 | Inhibition of human Nav 1.5 assessed as reduction in use dependent block at 1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302453 | Cmax in po dosed cynomolgus monkey | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1302494 | Inhibition of human Nav 1.6 assessed as reduction in use dependent block at 0.1 uM measured at 10 Hz by manual patch clamp assay | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346758 | Human Nav1.5 (Voltage-gated sodium channels) | 2018 | British journal of pharmacology, 06, Volume: 175, Issue:12
| Selective late sodium current inhibitor GS-458967 suppresses Torsades de Pointes by mostly affecting perpetuation but not initiation of the arrhythmia. |
| AID1346758 | Human Nav1.5 (Voltage-gated sodium channels) | 2016 | Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |