Basic Information
ID: ALA3888930
Type: Binding
Description: Inhibition Assay: The hERG inhibition study aims at quantifying the in vitro effects of compounds of the invention on the potassium-selective IKr current generated in normoxic conditions in stably transfected HEK 293 cells with the human ether-a-go-go-related gene (hERG). Whole-cell currents (acquisition by manual patch-clamp) elicited during a voltage pulse were recorded in baseline conditions and following application of tested compounds (5 minutes of exposure). The concentrations of tested compounds (0.3 μM; 3 μM; 10 μM; 30 μM) reflect a range believed to exceed the concentrations at expected efficacy doses in preclinical models. The pulses protocol applied is described as follow: the holding potential (every 3 seconds) was stepped from −80 mV to a maximum value of +40 mV, starting with −40 mV, in eight increments of +10 mV, for a period of 1 second. The membrane potential was then returned to −55 mV, after each of these incremented steps, for 1 second and finally repolarized to −80 mV for 1 second.
Organism: Homo sapiens
Cell type: Sf9
Activity Charts
Bioactivity
Activity Types for Assay ALA3888930
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 358.40 | 2.46 | 2.46 |
| 374.86 | 2.98 | 2.98 |
| 340.41 | 2.32 | 2.32 |
| 388.43 | 1.82 | 1.82 |
| 392.85 | 3.11 | 3.11 |
| 365.42 | 2.19 | 2.19 |
| 409.30 | 3.63 | 3.63 |
| 420.50 | 3.84 | 3.84 |
| 408.41 | 3.34 | 3.34 |
| 376.39 | 2.60 | 2.60 |
| 386.46 | 3.24 | 3.24 |
| 356.36 | 2.25 | 2.25 |
| 374.86 | 2.98 | 2.98 |
| 358.40 | 2.46 | 2.46 |
| 376.39 | 2.60 | 2.60 |
| 376.39 | 2.60 | 2.60 |
| 372.43 | 2.85 | 2.85 |
| 412.37 | 2.88 | 2.88 |
| 372.43 | 2.72 | 2.72 |
| 370.44 | 2.33 | 2.33 |
| 392.85 | 3.11 | 3.11 |
| 394.38 | 2.74 | 2.74 |
| 394.38 | 2.74 | 2.74 |