Basic Information
ID: ALA3707547
Type: Binding
Description: Radioligand Binding: Human or rat P2X7-1321N1 cells were collected and frozen @-80.degree. C. On the day of the experiment, cell membrane preparations were made according to standard published methods. The total assay volume was 100 .mu.l:10 .mu.l compound (10.times.)+(b) 40 .mu.l tracer (2.5.times.)+50 .mu.l membrane (2.times.). The tracer used for the assay was tritiated A-804598. The compound can be prepared as described in the literature. (Donnelly-Roberts, D. Neuropharmacology 2009, 56 (1), 223-229.) Compounds, tracer and membranes were incubated for 1 hour @ 4.degree. C. The assay was terminated by filtration (GF/B filters pre-soaked with 0.3% PEI) and washed with washing buffer (Tris-HCl 50 mM).
Cell type: P2X7-1321N1
Activity Charts
Bioactivity
Activity Types for Assay ALA3707547
Ki
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 448.84 | 4.16 | 4.16 |
| 453.88 | 4.82 | 4.82 |
| 465.84 | 4.90 | 4.90 |
| 461.88 | 5.07 | 5.07 |
| 477.87 | 4.77 | 4.77 |
| 447.85 | 4.76 | 4.76 |
| 450.82 | 5.12 | 5.12 |
| 433.82 | 4.37 | 4.37 |
| 434.81 | 3.77 | 3.77 |
| 451.81 | 4.51 | 4.51 |
| 413.40 | 4.03 | 4.03 |
| 451.81 | 4.51 | 4.51 |
| 434.81 | 3.77 | 3.77 |
| 419.25 | 3.54 | 3.54 |
| 433.82 | 4.37 | 4.37 |
| 439.85 | 4.43 | 4.43 |
| 452.80 | 3.91 | 3.91 |
| 436.83 | 4.01 | 4.01 |
| 457.84 | 4.57 | 4.57 |
| 419.43 | 4.09 | 4.09 |
| 424.29 | 4.21 | 4.21 |
| 473.31 | 5.69 | 5.69 |