# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3428402 | Binding | Inhibition of SYK (unknown origin) assessed as remaining activity at 100 uM by radioactive filter binding assay in presence of [33P]-ATP relative to control | Homo sapiens | 16 | ALA3425453 | single protein format | Scientific Literature | |
2. | ALA3583143 | Binding | Inhibition of Tel-fused SYK (unknown origin) expressed in mouse BA/F3 cells after 48 hrs by luciferase reporter gene assay in absence of recombinant mouse IL3 | Homo sapiens | 3 | ALA3580662 | cell-based format | Scientific Literature | |
3. | ALA3595082 | Binding | Inhibition of SYK (unknown origin) | Homo sapiens | 1 | ALA3593212 | single protein format | Scientific Literature | |
4. | ALA3606876 | Binding | Inhibition of SYK (unknown origin) at 2 uM by radioactive filter-binding assay | Homo sapiens | 1 | ALA3603808 | single protein format | Scientific Literature | |
5. | ALA3606895 | Binding | Inhibition of SYK (unknown origin) at 250 nM by radioactive filter-binding assay | Homo sapiens | 1 | ALA3603808 | single protein format | Scientific Literature | |
6. | ALA3606461 | Binding | Inhibition of human SYK | Homo sapiens | 1 | ALA3603755 | single protein format | Scientific Literature | |
7. | ALA3620014 | Binding | Inhibition of SYK (unknown origin) at 10 uM after 40 mins by scintillation counting analysis | Homo sapiens | 2 | ALA3616395 | single protein format | Scientific Literature | |
8. | ALA3620307 | Binding | Inhibition of SYK (unknown origin) after 40 mins by scintillation counting analysis | Homo sapiens | 1 | ALA3616395 | single protein format | Scientific Literature | |
9. | ALA3624367 | Binding | Inhibition of human recombinant Syk | Homo sapiens | 1 | ALA3621115 | single protein format | Scientific Literature | |
10. | ALA3627015 | Binding | Inhibition of purified full-length human SYK pre-incubated for 30 mins at room temperature before Ulight-TK peptide substrate addition and measured 1 hr after substrate addition by cell free kinase assay | Homo sapiens | 40 | ALA3621069 | single protein format | Scientific Literature | |
11. | ALA3627019 | Binding | Inhibition of SYK-mediated TNFalpha production in human IgG-stimulated human THP1 cells incubated for 18 hrs by ELISA method | Homo sapiens | 4 | ALA3621069 | cell-based format | Scientific Literature | |
12. | ALA3627026 | Binding | Inhibition of purified full-length human SYK at 0.1 uM pre-incubated for 30 mins at room temperature before Ulight-TK peptide substrate addition and measured 1 hr after substrate addition by cell free kinase assay | Homo sapiens | 1 | ALA3621069 | single protein format | Scientific Literature | |
13. | ALA3627027 | Binding | Inhibition of purified full-length human SYK at 0.01 uM pre-incubated for 30 mins at room temperature before Ulight-TK peptide substrate addition and measured 1 hr after substrate addition by cell free kinase assay | Homo sapiens | 1 | ALA3621069 | single protein format | Scientific Literature | |
14. | ALA3627444 | Binding | Inhibition of Syk (unknown origin) using 5-Fluo-Ahx-GAPDYENLQELNKK-Amide as substrate after 60 mins by microfluidic mobility shift assay | Homo sapiens | 13 | ALA3621151 | single protein format | Scientific Literature | |
15. | ALA3627445 | Binding | Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis | Homo sapiens | 13 | ALA3621151 | cell-based format | Scientific Literature | |
16. | ALA3627446 | Binding | Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes in presence of 90% human blood assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis | Homo sapiens | 13 | ALA3621151 | assay format | Scientific Literature | |
17. | ALA3631488 | Binding | Inhibition of SYK (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay | Homo sapiens | 3 | ALA3627608 | single protein format | Scientific Literature | |
18. | ALA3631695 | Binding | Inhibition of Syk (unknown origin) at 1 uM by FRET method | Homo sapiens | 1 | ALA3627690 | single protein format | Scientific Literature | |
19. | ALA3705225 | Binding | 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. | Homo sapiens | 46 | ALA3639355 | single protein format | BindingDB Database | |
20. | ALA3705362 | Binding | Mobility-Shift kinase assay: Compounds of the examples provided herein were assessed for their ability to inhibit Syk kinase by utilizing Caliper Life Sciences' proprietary LabChip technology. The off-chip incubation mobility-shift kinase assay uses a microfluidic chip to measure the conversion of a fluorescent peptide substrate to a phosphorylated product. The reaction mixture, from a microtiter plate well, is introduced through a capillary sipper onto the chip, where the nonphosphorylated substrate and phosphorylated product are separated by electrophoresis and detected via laser induced fluorescence. The signature of the fluorescence signal over time reveals the extent of the reaction. The phosphorylated product migrates through the chip faster than the non-phosphorylated substrate, and signals from the two forms of the peptide appear as distinct peaks. | Homo sapiens | 722 | ALA3639055 | single protein format | BindingDB Database |