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# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3428741 | Binding | Inhibition of p38alpha MAPK(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. | ALA3580221 | Binding | Inhibition of p38alpha MAP kinase (unknown origin) using GFP-ATF2 as substrate after 1 hr by TR-FRET assay | Homo sapiens | 21 | ALA3576835 | single protein format | Scientific Literature | |
3. | ALA3595483 | Binding | Inhibition of human MAPK14 at 0.1 uM relative to control | Homo sapiens | 1 | ALA3593229 | single protein format | Scientific Literature | |
4. | ALA3608085 | Binding | Inhibition of human P38alpha | Homo sapiens | 1 | ALA3603755 | single protein format | Scientific Literature | |
5. | ALA3624073 | Binding | Inhibition of MAPK1 (unknown origin) assessed as residual enzyme activity at 10 uM by kinaseprolier assay | Homo sapiens | 1 | ALA3621116 | single protein format | Scientific Literature | |
6. | ALA3624081 | Binding | Inhibition of Sapk2A (unknown origin) assessed as residual enzyme activity at 10 uM by kinaseprolier assay | Homo sapiens | 1 | ALA3621116 | single protein format | Scientific Literature | |
7. | ALA3630746 | Binding | Inhibition of P38alpha (unknown origin) at 10 uM after 120 mins P33 radiolabeled kinase activity assay | Homo sapiens | 3 | ALA3627608 | single protein format | Scientific Literature | |
8. | ALA3631180 | Binding | Inhibition of p38alpha (unknown origin) at 1 uM by FRET method | Homo sapiens | 1 | ALA3627690 | single protein format | Scientific Literature | |
9. | ALA3630849 | Binding | Inhibition of p38-alpha (unknown origin) assessed as remaining activity at 10 uM by high-throughput assay relative to control | Homo sapiens | 1 | ALA3627674 | single protein format | Scientific Literature | |
10. | ALA3635885 | Binding | Inhibition of human recombinant p38alpha expressed in Escherichia coli using ATF2 as substrate by proprietary radioisotopic protein kinase assay | Homo sapiens | 15 | ALA3632597 | assay format | Scientific Literature | |
11. | ALA3636794 | Binding | Inhibition of P38a (unknown origin) after 120 mins by HotSpot assay | Homo sapiens | 1 | ALA3632549 | single protein format | Scientific Literature | |
12. | ALA3705568 | Binding | Inhibition Assay: Using human p38 MAPK alpha , the p38 MAPK inhibitory activity of Compound (I) was studied by a method partially modified from the method described in Current Medicinal Chemistry (2004, No. 11, pp. 721-730).A solution of each test compound solution in 100% DMSO and a p38alpha /SAPK2a solution (Final Concentration: 1.5 nM) (Invitrogen) were added to a 384-well plate, and then the plate was incubated at room temperature in a dark place for 1 hour. Thereafter, ATP (Final Concentration: 100 uM), which is a phosphate donor, and biotinylated ATF2 (Final Concentration: 30 nM) (upstate), which is a substrate, were added, and the resulting mixture was allowed to react at room temperature in a dark place for 1 hour (the final concentration of DMSO was 0.25%). After the reaction, an anti-phosphorylated ATF2 antibody (Final Concentration: 1 nM) (Cell Signaling), anti-IgG acceptor beads (Final Concentration: 20 ug/mL) (PerkinElmer) and streptavidin donor beads. | Homo sapiens | 9 | ALA3638866 | single protein format | BindingDB Database | |
13. | ALA3706164 | Binding | Enzyme Inhibition Assay: The kinase enzyme binding activities of compounds disclosed herein were determined using a proprietary assay which measures active site-directed competition binding to an immobilized ligand (Fabian, M. A. et al., Nature Biotechnol., 2005, 23:329-336). These assays were conducted by DiscoverX (formerly Ambit; San Diego, Calif.). The Kd value (Dissociation constant value) was calculated as the index of affinity of the compounds to each kinase. The enzyme inhibitory activities of compounds disclosed herein were determined by FRET using synthetic peptides labelled with both donor and acceptor fluorophores (Z-LYTE, Invitrogen Ltd., Paisley, UK). The inhibitory activities of test compounds against the p38 MAPKalpha isoform (MAPK14: Invitrogen), were evaluated indirectly by determining the level of activation/phosphorylation of the down-stream molecule, MAPKAP-K2. The p38 MAPKalpha protein (80 ng/mL, 2.5 uL) was mixed with the test compound (2.5 uL of either 4 ug/mL, 0.4 & 0.04 ug/mL). | Homo sapiens | 1 | ALA3639240 | single protein format | BindingDB Database | |
14. | ALA3705800 | Binding | Inhibition Assay: Enzymatic activity assay was performed in 96-well microtiter plates (Corning, catalog number #3686) using a total volume of 50 ul of an assay buffer composed of 50 mM HEPES pH 7.5, 10 mM MgCl2, 1.75 mM Na3VO4. Various concentrations of the test compound or vehicle controls were pre-incubated for one hour with 0.055 ug/ml of the human p38alfa (SAPKa) enzyme (obtained from University of Dundee). The reaction was started by addition of biotinylated ATF2 substrate and ATP in concentrations around their Km values (final concentration 0.62 uM and 60 uM respectively) and took place for one hour at 25 C. Addition of the detection reagents, streptavidin XL665 and anti-phosphoresidue antibody coupled to Europium cryptate, caused the juxtaposition of the cryptate and the XL665 fluorophore, resulting in fluorescence energy transfer (FRET). The FRET intensity depends on the amount of bounded cryptate antibody, which is proportional to the extent of substrate phosphorylation. | Homo sapiens | 36 | ALA3638430 | single protein format | BindingDB Database | |
15. | ALA3706342 | Binding | Biological Assay: Kinase reaction buffer for p38alpha HTRF assays consists of 50 mM Tris-pH 7.5, 5 mM MgCl2, 0.1 mg/mL BSA, 100 uM Na3VO4 and 0.5 mM DTT. HTRF Detection Buffer:HTRF detection buffer contains 100 mM HEPES-pH 7.5, 100 mM NaCl, 0.1% BSA, 0.05% Tween-20, and 10 mM EDTA. Serial Dilution of Compounds: Compounds were dissolved in 100% DMSO and serially diluted (3 fold, 10 point) in a polypropylene 96-well microtiter plate (drug plate). The final starting concentration of compounds in the p38alpha enzymatic assays was 1 uM. Columns 6 and 12 (HI controls and LO controls respectively) in the drug plate were reserved as controls and contained only DMSO.Kinase Reaction: The p38alpha kinase reactions were carried out in a polypropylene 96-well black round bottom assay plate in total volume of 30 uL kinase reaction buffer. | Homo sapiens | 21 | ALA3639012 | single protein format | BindingDB Database | |
16. | ALA3705609 | Binding | Enzyme Inhibition Assay: The inhibitory activities of compounds of the invention against p38MAPKγ (MAPK12: Invitrogen) are evaluated in a similar fashion to that described hereinabove. The enzyme (800 ng/mL, 2.5 μL) is incubated with the test compound (2.5 μL of either 4 μg/mL, 0.4 μg/mL, 0.04 μg/mL, or 0.004 μg/mL) for 2 hr at RT. The FRET peptide (8 μM, 2.5 μL) and appropriate ATP solution (2.5 μL, 400 μM) are then added to the enzymes/compound mixtures and the whole is incubated for 1 hr. Development reagent (protease, 5 μL) is added for 1 hr prior to detection in a fluorescence microplate reader (Varioskan Flash, Thermo Scientific). | Homo sapiens | 1 | ALA3638580 | single protein format | BindingDB Database | |
17. | ALA3705477 | Binding | Fluorescence Resonance Energy Transfer (FRET) Assay: The enzyme inhibitory activity of test compounds was determined by fluorescence resonance energy transfer (FRET) using synthetic peptides labelled with both donor and acceptor fluorophores (Z-LYTE, Invitrogen). Recombinant, phosphorylated p38 MAPK (MAPK12:Millipore) was diluted in HEPES buffer, mixed with compound at the desired final concentrations and incubated for 2 hr at RT. The FRET peptide (2 uM) and ATP (100 uM) were next added to the enzyme/compound mixture and incubated for 1 hr. Development reagent (protease) was added for 1 hr prior to detection in a fluorescence microplate reader. The site-specific protease only cleaves non-phosphorylated peptide and eliminates the FRET signal. Phosphorylation levels of each reaction were calculated using the ratio of coumarin emission (donor) over fluorescein emission (acceptor) with high ratios indicating high phosphorylation levels and low ratios indicating low phosphorylation levels. | Homo sapiens | 36 | ALA3639041 | single protein format | BindingDB Database | |
18. | ALA3734491 | Binding | Inhibition of recombinant human P38alpha using fluorescein-labeled peptide as substrate by fluorescence-electrophoretic mobility shift assay | Homo sapiens | 1 | ALA3727354 | single protein format | Patent Bioactivity Data | |
19. | ALA3737486 | Binding | Inhibition of p38 alpha (unknown origin) at 1 uM by selectscreen kinase profiling assay in presence of ATP | Homo sapiens | 1 | ALA3734692 | single protein format | Scientific Literature | |
20. | ALA3739153 | Binding | Inhibition of p38alpha (unknown origin) at 200 nM by electrophoretic mobility shift assay | Homo sapiens | 2 | ALA3734671 | single protein format | Scientific Literature |