Basic Information
ID: ALA3705806
Type: Binding
Description: Biochemical Assay: Through the Molecular Library Probe Production Center Network (MLPCN), at least 300,000 compounds were screened using a TR-FRET method, an ALPHASCREEN method or both, and tested for their ability to inhibit SUMOylation of a target protein via SUMO E1 or SUMO E2. The assays were based on SUMOylation of the target protein RanGAP1, which is a protein that is efficiently SUMOylated with only the SUMO E1 and E2 enzymes, and does not use E3 ligases. A fluorescence resonance energy transfer (FRET) assay was the primary assay followed by a chemoluminescence-based secondary assay using ALPHA screen to eliminate false positive hits. Then, the hits were screened by a poly-ubiquitination assay using ubiquitin, ubiquitin E1, Ubc5 and Apc11 to eliminate inhibitors not specific to SUMOylation. The screening identified a potent family of SUMOylation inhibitors based on a tricyclic scaffold.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705806
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 437.89 | 5.41 | 5.41 |
| 307.36 | 3.21 | 3.21 |
| 534.66 | 5.33 | 5.33 |
| 387.42 | 4.65 | 4.65 |
| 369.43 | 4.51 | 4.51 |
| 403.87 | 5.16 | 5.16 |
| 518.62 | 4.71 | 4.71 |
| 380.47 | 3.80 | 3.80 |
| 484.58 | 5.47 | 5.47 |
| 431.93 | 5.78 | 5.78 |
| 512.01 | 6.07 | 6.07 |
| 359.39 | 4.10 | 4.10 |
| 519.03 | 6.12 | 6.12 |