Basic Information
ID: ALA3707743
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 ALA3707743
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 415.91 | 3.76 | 3.76 |
| 483.01 | 3.95 | 3.95 |
| 399.46 | 3.25 | 3.25 |
| 403.90 | 3.62 | 3.62 |
| 401.89 | 3.37 | 3.37 |
| 403.90 | 3.62 | 3.62 |
| 429.94 | 4.15 | 4.15 |
| 403.90 | 3.76 | 3.76 |
| 403.90 | 3.62 | 3.62 |
| 335.78 | 2.35 | 2.35 |
| 433.90 | 3.86 | 3.86 |
| 414.93 | 3.80 | 3.80 |
| 397.92 | 3.62 | 3.62 |
| 411.95 | 4.01 | 4.01 |
| 397.86 | 3.84 | 3.84 |
| 443.97 | 4.54 | 4.54 |
| 444.96 | 3.61 | 3.61 |
| 428.91 | 2.87 | 2.87 |
| 431.91 | 2.88 | 2.88 |
| 429.94 | 4.15 | 4.15 |
| 430.93 | 3.22 | 3.22 |
| 432.95 | 3.47 | 3.47 |
| 377.87 | 3.52 | 3.52 |
| 404.53 | 3.24 | 3.24 |
| 450.58 | 3.66 | 3.66 |
| 478.59 | 2.95 | 2.95 |
| 451.56 | 3.35 | 3.35 |
| 465.59 | 4.00 | 4.00 |
| 403.54 | 3.70 | 3.70 |
| 482.96 | 3.84 | 3.84 |
| 421.53 | 3.99 | 3.99 |
| 442.38 | 3.73 | 3.73 |
| 436.55 | 3.49 | 3.49 |
| 462.59 | 3.98 | 3.98 |
| 430.93 | 3.27 | 3.27 |
| 456.97 | 3.75 | 3.75 |
| 459.97 | 3.78 | 3.78 |
| 479.40 | 3.97 | 3.97 |
| 432.82 | 3.13 | 3.13 |
| 403.54 | 3.85 | 3.85 |
| 480.94 | 3.86 | 3.86 |
| 444.96 | 3.47 | 3.47 |
| 431.84 | 3.92 | 3.92 |
| 417.81 | 3.67 | 3.67 |
| 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 |
| 451.89 | 4.01 | 4.01 |
| 405.44 | 3.60 | 3.60 |
| 480.60 | 3.24 | 3.24 |
| 492.61 | 3.60 | 3.60 |
| 498.57 | 4.22 | 4.22 |
| 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 |
| 487.60 | 3.73 | 3.73 |
| 501.54 | 4.80 | 4.80 |
| 438.57 | 3.98 | 3.98 |
| 494.60 | 4.32 | 4.32 |
| 445.50 | 4.52 | 4.52 |
| 460.52 | 3.98 | 3.98 |
| 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 |
| 428.50 | 3.43 | 3.43 |
| 425.52 | 3.37 | 3.37 |
| 506.64 | 3.73 | 3.73 |
| 436.55 | 3.73 | 3.73 |
| 397.39 | 3.26 | 3.26 |
| 437.46 | 4.14 | 4.14 |
| 430.93 | 3.51 | 3.51 |
| 478.51 | 3.93 | 3.93 |
| 423.43 | 3.89 | 3.89 |
| 408.28 | 3.76 | 3.76 |
| 444.74 | 4.20 | 4.20 |
| 436.55 | 3.90 | 3.90 |
| 393.48 | 3.49 | 3.49 |
| 408.50 | 2.95 | 2.95 |
| 367.44 | 2.96 | 2.96 |
| 506.64 | 3.99 | 3.99 |
| 460.52 | 3.98 | 3.98 |
| 408.50 | 2.95 | 2.95 |
| 367.44 | 2.96 | 2.96 |
| 413.85 | 3.65 | 3.65 |
| 433.90 | 3.90 | 3.90 |
| 474.96 | 3.89 | 3.89 |
| 425.50 | 3.69 | 3.69 |
| 438.57 | 3.98 | 3.98 |
| 417.45 | 3.60 | 3.60 |
| 461.50 | 3.61 | 3.61 |
| 443.49 | 4.13 | 4.13 |
| 458.50 | 3.59 | 3.59 |
| 444.96 | 3.90 | 3.90 |
| 415.91 | 4.05 | 4.05 |
| 438.86 | 2.83 | 2.83 |
| 423.84 | 3.37 | 3.37 |
| 448.56 | 3.74 | 3.74 |
| 506.64 | 3.99 | 3.99 |
| 462.59 | 3.87 | 3.87 |
| 474.96 | 3.89 | 3.89 |
| 456.97 | 3.75 | 3.75 |
| 415.91 | 3.76 | 3.76 |
| 433.90 | 3.90 | 3.90 |
| 435.44 | 4.04 | 4.04 |
| 429.82 | 3.81 | 3.81 |
| 450.45 | 3.49 | 3.49 |
| 444.83 | 3.27 | 3.27 |
| 436.91 | 3.46 | 3.46 |
| 433.55 | 4.13 | 4.13 |
| 466.55 | 3.68 | 3.68 |
| 451.54 | 4.22 | 4.22 |
| 448.56 | 3.59 | 3.59 |
| 432.46 | 3.34 | 3.34 |
| 417.45 | 3.88 | 3.88 |
| 426.84 | 3.12 | 3.12 |
| 411.83 | 3.66 | 3.66 |
| 381.47 | 3.49 | 3.49 |
| 422.52 | 3.49 | 3.49 |
| 417.45 | 3.45 | 3.45 |
| 443.49 | 3.99 | 3.99 |
| 458.50 | 3.44 | 3.44 |
| 436.55 | 3.73 | 3.73 |
| 407.51 | 3.60 | 3.60 |
| 442.53 | 3.68 | 3.68 |
| 431.91 | 3.14 | 3.14 |
| 465.37 | 3.88 | 3.88 |
| 465.59 | 3.86 | 3.86 |
| 435.52 | 3.24 | 3.24 |
| 420.51 | 3.78 | 3.78 |
| 394.47 | 3.25 | 3.25 |
| 424.54 | 3.73 | 3.73 |
| 383.49 | 3.74 | 3.74 |
| 423.55 | 4.66 | 4.66 |
| 449.59 | 5.20 | 5.20 |
| 409.52 | 4.27 | 4.27 |
| 464.60 | 4.66 | 4.66 |
| 442.53 | 3.68 | 3.68 |
| 450.58 | 4.12 | 4.12 |
| 361.82 | 2.90 | 2.90 |
| 399.82 | 3.37 | 3.37 |
| 363.84 | 3.02 | 3.02 |
| 389.88 | 3.55 | 3.55 |
| 404.89 | 3.01 | 3.01 |
| 424.54 | 3.59 | 3.59 |
| 409.52 | 4.13 | 4.13 |
| 472.97 | 3.13 | 3.13 |
| 442.94 | 3.69 | 3.69 |
| 479.40 | 4.13 | 4.13 |
| 498.57 | 4.22 | 4.22 |
| 483.55 | 4.77 | 4.77 |
| 457.51 | 4.23 | 4.23 |
| 355.43 | 3.10 | 3.10 |
| 549.67 | 4.48 | 4.48 |
| 534.65 | 5.03 | 5.03 |
| 523.63 | 4.00 | 4.00 |
| 501.00 | 3.90 | 3.90 |
| 424.54 | 3.59 | 3.59 |
| 435.56 | 4.66 | 4.66 |
| 450.58 | 4.12 | 4.12 |
| 381.47 | 3.21 | 3.21 |
| 407.51 | 3.74 | 3.74 |
| 440.51 | 3.15 | 3.15 |
| 438.57 | 3.83 | 3.83 |
| 432.95 | 3.61 | 3.61 |
| 417.93 | 4.15 | 4.15 |
| 476.61 | 4.22 | 4.22 |
| 403.90 | 3.91 | 3.91 |
| 446.49 | 3.59 | 3.59 |
| 405.44 | 3.60 | 3.60 |
| 420.45 | 3.10 | 3.10 |
| 409.52 | 4.13 | 4.13 |
| 409.52 | 4.13 | 4.13 |
| 383.49 | 3.60 | 3.60 |
| 448.56 | 3.90 | 3.90 |
| 421.53 | 3.84 | 3.84 |
| 478.59 | 3.36 | 3.36 |
| 407.51 | 4.05 | 4.05 |
| 409.52 | 4.13 | 4.13 |
| 424.54 | 3.59 | 3.59 |
| 419.47 | 3.99 | 3.99 |
| 460.52 | 3.98 | 3.98 |
| 472.97 | 3.13 | 3.13 |
| 486.56 | 4.37 | 4.37 |
| 451.48 | 4.53 | 4.53 |
| 477.52 | 5.06 | 5.06 |
| 492.54 | 4.52 | 4.52 |
| 463.49 | 4.67 | 4.67 |
| 478.51 | 4.13 | 4.13 |
| 422.52 | 3.20 | 3.20 |
| 508.62 | 4.49 | 4.49 |
| 463.49 | 4.82 | 4.82 |
| 446.49 | 3.59 | 3.59 |
| 363.84 | 3.13 | 3.13 |
| 369.46 | 3.35 | 3.35 |
| 410.51 | 3.34 | 3.34 |
| 436.33 | 3.73 | 3.73 |
| 501.00 | 3.90 | 3.90 |
| 483.01 | 3.95 | 3.95 |
| 466.55 | 3.68 | 3.68 |
| 403.90 | 3.76 | 3.76 |
| 467.99 | 4.49 | 4.49 |
| 441.95 | 3.96 | 3.96 |