Assay Report Card

Basic Information

ID: ALA3887284

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 um 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.

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
390.374.224.22
446.423.783.78
381.332.342.34
450.405.585.58
437.815.175.17
434.383.923.92
422.354.054.05
504.454.224.22
484.394.714.71
429.414.704.70
414.404.694.69
433.404.524.52
503.464.834.83
471.904.724.72
456.433.603.60
386.373.773.77
518.474.264.26
434.383.923.92
419.463.933.93
404.363.913.91
468.473.473.47
415.384.094.09
432.413.923.92
479.513.943.94
444.444.994.99
467.484.074.07
452.374.374.37
415.384.094.09
470.364.674.67
434.383.923.92
450.844.434.43
468.924.284.28
484.923.983.98
379.353.553.55
517.494.874.87
483.934.594.59
445.413.993.99
429.414.704.70
468.473.473.47
455.444.214.21
483.934.594.59
452.473.773.77
438.804.564.56
418.384.224.22
484.923.983.98
482.493.733.73
472.894.114.11
429.414.704.70
416.415.435.43
390.374.224.22
380.342.942.94
480.503.343.34
469.385.275.27
376.353.503.50
437.454.074.07
420.375.265.26
414.404.694.69
415.384.094.09
467.934.894.89
486.463.923.92
379.353.553.55
434.844.734.73
434.383.923.92
467.484.074.07
451.484.374.37
450.844.434.43
432.413.923.92
459.444.194.19
421.364.654.65
470.364.674.67
420.453.323.32
430.404.094.09
438.443.463.46
485.474.534.53
467.484.234.23
468.473.473.47
440.413.983.98
467.484.074.07
457.434.004.00
424.343.513.51