Basic Information
ID: ALA3706105
Type: Binding
Description: Electrophysiology Assay: Patch clamp electrophysiology was used to assess the efficacy and selectivity of sodium channel blockers in dorsal root ganglion neurons. Rat neurons were isolated from the dorsal root ganglions and maintained in culture for 2 to 10 days in the presence of NGF (50 ng/ml) (culture media consisted of NeurobasalA supplemented with B27, glutamine and antibiotics). Small diameter neurons (nociceptors, 8-12 μm in diameter) were visually identified and probed with fine tip glass electrodes connected to an amplifier (Axon Instruments). The voltage clamp mode was used to assess the compound's IC50 holding the cells at −60 mV. In addition, the current clamp mode was employed to test the efficacy of the compounds in blocking action potential generation in response to current injections. The results of these experiments contributed to the definition of the efficacy profile of the compounds.
Tissue: Dorsal root ganglion
Activity Charts
Bioactivity
Activity Types for Assay ALA3706105
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 503.78 | 6.88 | 6.88 |
| 487.33 | 6.36 | 6.36 |
| 483.36 | 6.53 | 6.53 |
| 453.77 | 6.24 | 6.24 |
| 433.36 | 5.90 | 5.90 |
| 437.32 | 5.73 | 5.73 |
| 485.34 | 6.35 | 6.35 |
| 505.32 | 6.75 | 6.75 |
| 501.35 | 6.91 | 6.91 |
| 517.35 | 6.61 | 6.61 |
| 487.33 | 6.61 | 6.61 |
| 450.25 | 5.88 | 5.88 |
| 420.22 | 5.88 | 5.88 |
| 434.25 | 6.18 | 6.18 |
| 402.23 | 5.74 | 5.74 |
| 450.25 | 5.37 | 5.37 |
| 500.26 | 6.68 | 6.68 |
| 466.70 | 6.40 | 6.40 |
| 468.24 | 6.34 | 6.34 |
| 450.71 | 6.70 | 6.70 |
| 462.29 | 5.24 | 5.24 |
| 450.25 | 5.37 | 5.37 |
| 454.67 | 6.53 | 6.53 |
| 438.21 | 6.01 | 6.01 |
| 466.70 | 5.88 | 5.88 |
| 486.23 | 6.63 | 6.63 |
| 499.36 | 6.23 | 6.23 |
| 433.36 | 5.90 | 5.90 |
| 421.21 | 5.27 | 5.27 |
| 489.36 | 6.56 | 6.56 |
| 435.24 | 5.58 | 5.58 |
| 403.22 | 5.13 | 5.13 |
| 451.24 | 4.76 | 4.76 |
| 501.24 | 6.07 | 6.07 |
| 467.69 | 5.79 | 5.79 |
| 469.23 | 5.73 | 5.73 |
| 451.69 | 6.09 | 6.09 |
| 463.27 | 4.63 | 4.63 |
| 451.24 | 4.76 | 4.76 |
| 455.66 | 5.92 | 5.92 |
| 439.20 | 5.41 | 5.41 |
| 467.69 | 5.28 | 5.28 |
| 487.22 | 6.03 | 6.03 |
| 500.35 | 5.87 | 5.87 |
| 500.35 | 5.35 | 5.35 |
| 502.34 | 6.31 | 6.31 |
| 518.34 | 6.01 | 6.01 |
| 530.38 | 5.36 | 5.36 |
| 488.31 | 6.00 | 6.00 |
| 451.24 | 5.28 | 5.28 |
| 438.46 | 5.27 | 5.27 |
| 422.46 | 5.57 | 5.57 |
| 408.43 | 5.26 | 5.26 |
| 352.32 | 3.96 | 3.96 |
| 420.32 | 4.98 | 4.98 |
| 450.34 | 4.99 | 4.99 |
| 454.76 | 5.64 | 5.64 |
| 450.34 | 4.99 | 4.99 |
| 468.33 | 5.44 | 5.44 |
| 450.80 | 5.81 | 5.81 |
| 432.35 | 4.85 | 4.85 |
| 436.77 | 5.50 | 5.50 |
| 460.41 | 5.63 | 5.63 |
| 462.38 | 4.34 | 4.34 |
| 466.80 | 5.51 | 5.51 |
| 446.38 | 4.64 | 4.64 |
| 466.80 | 4.99 | 4.99 |
| 450.34 | 4.99 | 4.99 |
| 402.33 | 4.84 | 4.84 |
| 420.32 | 4.98 | 4.98 |
| 500.35 | 5.63 | 5.63 |
| 470.32 | 5.62 | 5.62 |
| 454.76 | 5.64 | 5.64 |
| 434.35 | 5.29 | 5.29 |