Basic Information
ID: ALA3705225
Type: Binding
Description: Homogeneous Time-Resolved Fluorescence (HTRF) Assay : A recombinant GST-hSYK fusion protein was used to measure potency of compounds to inhibit human SYK activity. The recombinant human GST-SYK (Carna Biosciences #08-176) (5 pM final concentration) was incubated with various concentrations of the inhibitor diluted in DMSO (0.1% final concentration) for 10 minutes at room temperature in 15 mM Tris-HCl (pH 7.5), 0.01% tween 20, 2 mM DTT in 384 well plate format. To initiate the reaction the biotinylated substrate peptide (250 nM final concentration) that contains the phosphorylation site for SYK was added with magnesium (5 mM final concentration) and ATP (25 μM final concentration). Final volume of the reaction was 10 μL. Phosphorylation of the peptide was allowed to proceed for 45′ at room temperature.
Organism: Homo sapiens
Activity Charts
Bioactivity
Activity Types for Assay ALA3705225
IC50
Compound Summary
| Parent Molecular Weight | ALogP | Polar Surface Area |
|---|---|---|
| 500.50 | 5.62 | 5.62 |
| 532.59 | 6.34 | 6.34 |
| 507.54 | 5.11 | 5.11 |
| 487.03 | 5.49 | 5.49 |
| 528.68 | 6.30 | 6.30 |
| 450.45 | 3.33 | 3.33 |
| 453.45 | 2.75 | 2.75 |
| 480.63 | 5.46 | 5.46 |
| 390.44 | 3.00 | 3.00 |
| 653.81 | 6.69 | 6.69 |
| 536.58 | 5.78 | 5.78 |
| 452.58 | 5.06 | 5.06 |
| 394.54 | 5.32 | 5.32 |
| 666.65 | 6.70 | 6.70 |
| 490.63 | 4.61 | 4.61 |
| 497.62 | 3.52 | 3.52 |
| 562.62 | 4.50 | 4.50 |
| 402.40 | 5.06 | 5.06 |
| 520.48 | 6.60 | 6.60 |
| 526.97 | 6.11 | 6.11 |
| 584.61 | 7.03 | 7.03 |
| 492.63 | 5.84 | 5.84 |
| 408.41 | 4.69 | 4.69 |
| 460.49 | 5.57 | 5.57 |
| 462.46 | 3.24 | 3.24 |
| 487.55 | 5.93 | 5.93 |
| 506.55 | 5.77 | 5.77 |
| 432.43 | 4.18 | 4.18 |
| 472.52 | 3.05 | 3.05 |
| 463.49 | 4.77 | 4.77 |
| 478.50 | 5.22 | 5.22 |
| 384.53 | 4.75 | 4.75 |
| 501.44 | 4.77 | 4.77 |
| 477.51 | 4.57 | 4.57 |
| 534.56 | 3.45 | 3.45 |
| 630.74 | 5.81 | 5.81 |
| 492.52 | 5.38 | 5.38 |
| 520.58 | 6.42 | 6.42 |
| 506.55 | 5.77 | 5.77 |
| 377.52 | 4.87 | 4.87 |
| 517.58 | 5.42 | 5.42 |
| 492.57 | 5.68 | 5.68 |
| 534.60 | 6.25 | 6.25 |
| 476.53 | 4.17 | 4.17 |
| 484.60 | 5.78 | 5.78 |
| 484.60 | 5.78 | 5.78 |