Assay Detail
Binding
CHEMBL3705225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
48
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Aminopyrimidines as SYK inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 7.65 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3685804 | — | — | 1 | 9.00 |
| CHEMBL3685806 | — | — | 1 | 9.00 |
| CHEMBL3685796 | MRL-SYKi | — | 1 | 9.00 |
| CHEMBL3685820 | — | — | 1 | 9.00 |
| CHEMBL3685821 | — | — | 2 | 9.00 |
| CHEMBL3685786 | — | — | 1 | 9.00 |
| CHEMBL3685822 | — | — | 1 | 8.70 |
| CHEMBL3685823 | — | — | 1 | 8.70 |
| CHEMBL3685819 | — | — | 1 | 8.70 |
| CHEMBL3685815 | — | — | 2 | 8.70 |
| CHEMBL3685799 | — | — | 1 | 8.70 |
| CHEMBL3685824 | — | — | 1 | 8.52 |
| CHEMBL3685807 | — | — | 1 | 8.52 |
| CHEMBL3685800 | — | — | 1 | 8.52 |
| CHEMBL3685825 | — | — | 1 | 8.40 |
| CHEMBL3685813 | — | — | 1 | 8.30 |
| CHEMBL3685801 | — | — | 1 | 8.22 |
| CHEMBL3685808 | — | — | 1 | 8.15 |
| CHEMBL3685790 | — | — | 1 | 7.96 |
| CHEMBL3685814 | — | — | 1 | 7.92 |
| CHEMBL3685826 | — | — | 1 | 7.89 |
| CHEMBL3685818 | — | — | 1 | 7.89 |
| CHEMBL3685817 | — | — | 1 | 7.82 |
| CHEMBL3685795 | — | — | 1 | 7.70 |
| CHEMBL3685802 | — | — | 1 | 7.68 |
| CHEMBL3685793 | — | — | 1 | 7.66 |
| CHEMBL3685816 | — | — | 1 | 7.62 |
| CHEMBL3685797 | — | — | 1 | 7.60 |
| CHEMBL3685791 | — | — | 1 | 7.58 |
| CHEMBL3685827 | — | — | 1 | 7.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3685806 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685796 | MRL-SYKi | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685786 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685820 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685804 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685821 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3685819 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3685822 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3685815 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3685823 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3685799 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3685824 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3685800 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3685807 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3685825 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3685815 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3685813 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3685801 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3685808 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3685790 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3685814 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3685818 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3685826 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3685817 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3685795 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3685802 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3685793 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3685816 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3685797 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3685791 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3685827 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3685828 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3685798 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL3685812 | — | IC50 | = | 237.0 | nM | 6.62 |
| CHEMBL3685809 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL3685789 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL3685787 | — | IC50 | = | 628.0 | nM | 6.20 |
| CHEMBL3685810 | — | IC50 | = | 1253.0 | nM | 5.90 |
| CHEMBL3685805 | — | IC50 | = | 2427.0 | nM | 5.62 |
| CHEMBL3685788 | — | IC50 | = | 3285.0 | nM | 5.48 |
| CHEMBL3685794 | — | IC50 | = | 5912.0 | nM | 5.23 |
| CHEMBL3685803 | — | IC50 | = | 6079.0 | nM | 5.22 |
| CHEMBL3685792 | — | IC50 | = | 8887.0 | nM | 5.05 |
| CHEMBL3685811 | MK-8457 | IC50 | < | 0.5 | nM | - |
| CHEMBL3685785 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3685821 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3685829 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3685830 | — | IC50 | < | 0.5 | nM | - |