Basic Information
ID: ALA3705543
Type: Binding
Description: 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.
Cell type: HEK293
Activity Charts
Bioactivity
Activity Types for Assay ALA3705543
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 415.91 | 3.76 | 3.76 |
| 483.01 | 3.95 | 3.95 |
| 403.90 | 3.62 | 3.62 |
| 444.96 | 3.61 | 3.61 |
| 404.53 | 3.24 | 3.24 |
| 478.59 | 2.95 | 2.95 |
| 465.59 | 4.00 | 4.00 |
| 482.96 | 3.84 | 3.84 |
| 421.53 | 3.99 | 3.99 |
| 442.38 | 3.73 | 3.73 |
| 462.59 | 3.98 | 3.98 |
| 403.54 | 3.85 | 3.85 |
| 480.94 | 3.86 | 3.86 |
| 430.93 | 3.22 | 3.22 |
| 415.91 | 3.62 | 3.62 |
| 441.95 | 4.30 | 4.30 |
| 492.61 | 3.34 | 3.34 |
| 447.57 | 4.52 | 4.52 |
| 480.58 | 3.93 | 3.93 |
| 457.51 | 4.23 | 4.23 |
| 492.61 | 3.61 | 3.61 |
| 498.57 | 4.22 | 4.22 |
| 405.44 | 3.60 | 3.60 |
| 480.60 | 3.24 | 3.24 |
| 492.61 | 3.60 | 3.60 |
| 413.51 | 3.37 | 3.37 |
| 462.59 | 3.83 | 3.83 |
| 475.50 | 4.26 | 4.26 |
| 431.48 | 4.13 | 4.13 |
| 516.56 | 4.25 | 4.25 |
| 478.51 | 4.28 | 4.28 |
| 501.54 | 4.80 | 4.80 |
| 464.48 | 3.88 | 3.88 |
| 483.55 | 4.77 | 4.77 |
| 422.52 | 3.34 | 3.34 |
| 445.59 | 3.23 | 3.23 |
| 448.59 | 3.26 | 3.26 |
| 508.62 | 4.49 | 4.49 |
| 463.49 | 4.82 | 4.82 |
| 446.49 | 3.59 | 3.59 |
| 369.46 | 3.35 | 3.35 |
| 410.51 | 3.34 | 3.34 |