| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3705543 | B | Electrophysiological Assay: Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and allows the determination of the time- and voltage-dependence of block which has been interpreted as differential binding to the resting, open, and inactivated states of the sodium channel (Hille, B., Journal of General Physiology (1977), 69: 497-515).The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney cells (HEK), permanently transfected with an expression vector containing the full-length cDNA coding for the desired human sodium channel alpha -subunit, grown in culture media containing 10% FBS, 1% PSG, and 0.5 mg/mL G418 at 37 C. with 5% CO2. HEK cells used for the electrophysiology (EP) recordings had a passage number of less than 40 for all studies and were used within three days from the time of plating. | 42 | ALA3638545 | cell-based format | BindingDB Database | ||
| 2. | ALA3705617 | B | Radioligand Binding Assay: Radioligand Binding Studies: Saturation experiments. A representative compound of formula (I) was tritiated. Three tritiums were incorporated in place of methyl hydrogens to generate [3H]compound. Binding of this radioligand was preformed in 5 mL borosilicate glass test tubes at room temperature. Binding was initiated by adding membranes to increasing concentrations of [3H]compound in 100 mM NaCl, 20 mM Tris HCl, pH 7.4 buffer containing 0.01% w/v bovine serum albumin (BSA) for 18 h. Non-specific binding was determined in the presence of 1 uM unlabelled compound. After 18 h, the reactants were filtered through GF/C glass fiber filters presoaked in 0.5% w/v polyethylene imine. Filters were washed with 15 mL ice cold 100 mM NaCl, 20 mM Tris HCl, pH7.4 buffer containing 0.25% BSA to separate bound from free ligand. [3H]compound bound to filters was quantified by liquid scintillation counting.Competitive binding experiments. | 398 | ALA3638545 | assay format | BindingDB Database | ||
| 3. | ALA3707743 | B | Electrophysiological Assay: Patch voltage clamp electrophysiology allows for the direct measurement and quantification of block of voltage-gated sodium channels (NaV's), and allows the determination of the time- and voltage-dependence of block which has been interpreted as differential binding to the resting, open, and inactivated states of the sodium channel (Hille, B., Journal of General Physiology (1977), 69: 497-515).The following patch voltage clamp electrophysiology studies were performed on representative compounds of the invention using human embryonic kidney cells (HEK), permanently transfected with an expression vector containing the full-length cDNA coding for the desired human sodium channel alpha -subunit, grown in culture media containing 10% FBS, 1% PSG, and 0.5 mg/mL G418 at 37 C. with 5% CO2. HEK cells used for the electrophysiology (EP) recordings had a passage number of less than 40 for all studies and were used within three days from the time of plating. | 210 | ALA3638545 | cell-based format | BindingDB Database | ||
| 4. | ALA4266768 | B | Inhibition of Nav1.7 (unknown origin) by electrophysiology assay | Homo sapiens | 2 | ALA4265883 | single protein format | Scientific Literature | |
| 5. | ALA4266781 | B | Selectivity ratio of IC50 for Nav1.5 (unknown origin) to IC50 for Nav1.7 (unknown origin) | Homo sapiens | 1 | ALA4265883 | assay format | Scientific Literature | |
| 6. | ALA4321987 | B | Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 15 | ALA4321785 | cell-based format | Scientific Literature | |
| 7. | ALA4321991 | B | Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 11 | ALA4321785 | cell-based format | Scientific Literature | |
| 8. | ALA4321992 | B | Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 12 | ALA4321785 | cell-based format | Scientific Literature | |
| 9. | ALA4321995 | B | Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 14 | ALA4321785 | cell-based format | Scientific Literature | |
| 10. | ALA4321996 | B | Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 13 | ALA4321785 | cell-based format | Scientific Literature | |
| 11. | ALA4321998 | B | Selectivity index, ratio of IC50 for inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 11 | ALA4321785 | cell-based format | Scientific Literature | |
| 12. | ALA4321999 | B | Selectivity index, ratio of IC50 for inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 12 | ALA4321785 | cell-based format | Scientific Literature | |
| 13. | ALA4322002 | B | Selectivity index, ratio of IC50 for inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 14 | ALA4321785 | cell-based format | Scientific Literature | |
| 14. | ALA4322003 | B | Selectivity index, ratio of IC50 for inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay to IC50 for inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay | Homo sapiens | 13 | ALA4321785 | cell-based format | Scientific Literature | |
| 15. | ALA4725212 | T | Incucyte cell viability with HEK293T | Homo sapiens | 1,713 | ALA4689842 | cell-based format | EUbOPEN Chemogenomic Library | |
| 16. | ALA4725213 | T | Incucyte cell viability with human fibroblast | Homo sapiens | 1,718 | ALA4689842 | cell-based format | EUbOPEN Chemogenomic Library | |
| 17. | ALA4725214 | T | Incucyte cell viability with U2OS | Homo sapiens | 1,712 | ALA4689842 | cell-based format | EUbOPEN Chemogenomic Library | |
| 18. | ALA5055691 | B | Displacement of [3H]GX-545 Nav1.7 (unknown origin) expressed in HEK cells by liquid scintillation counting based radioligand competition assay | Homo sapiens | 17 | ALA5055616 | cell-based format | Scientific Literature | |
| 19. | ALA5055692 | B | Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 1 hr in presence of veratridine by sodium influx assay | Homo sapiens | 17 | ALA5055616 | cell-based format | Scientific Literature | |
| 20. | ALA5055693 | B | Inhibition of human Nav1.5 expressed in HEK293 cells incubated for 1 hr in presence of veratridine and anthropleurin-C by sodium influx assay | Homo sapiens | 17 | ALA5055616 | cell-based format | Scientific Literature |
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