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# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3880355 | Binding | Inhibition of TAK1 in human A549 cells assessed as decrease in recombinant human IL-1beta-stimulated IL6 production at 50 uM preincubated for 3 hrs followed by IL-1beta stimulation measured after 18 hrs relative to control | Homo sapiens | 32 | ALA3879912 | cell-based format | Patent Bioactivity Data | |
2. | ALA3880356 | Binding | Inhibition of kinase tracer-236 binding to full length recombinant human His-tagged TAK1-TAB1 expressed in baculovirus by FRET assay | Homo sapiens | 36 | ALA3879912 | assay format | Patent Bioactivity Data | |
3. | ALA3880357 | Binding | Inhibition of TAK1 in human A549 cells assessed as decrease in recombinant human IL-1beta-stimulated IL6 production at 5 uM preincubated for 3 hrs followed by IL-1beta stimulation measured after 18 hrs relative to control | Homo sapiens | 32 | ALA3879912 | cell-based format | Patent Bioactivity Data | |
4. | ALA3880358 | Binding | Inhibition of TAK1 in human A549 cells assessed as decrease in recombinant human IL-1beta-stimulated IL6 production preincubated for 3 hrs followed by IL-1beta stimulation measured after 18 hrs | Homo sapiens | 26 | ALA3879912 | cell-based format | Patent Bioactivity Data | |
5. | ALA3889256 | Binding | Biological Assay: TAK1-TAB1 Binding Inhibitory Potency: The ability of candidate compounds to interact with TAK1-TAB1 is quantitated by a competitive binding assay using the LanthaScreen technology developed by Life Technologies. This assay is based on the binding of a proprietary, Alexa Fluor 647-labeled, ATP-competitive kinase inhibitor (kinase tracer-236) to the TAK1-TAB1 construct in presence of a europium-conjugated antibody, resulting in a FRET (fluorescence resonance energy transfer) signal. Displacement of the kinase tracer by compound results in a lower emission ratio upon excitation of the europium chelate. Candidate compounds are designed as potential irreversible inhibitors of TAK1-TAB1, capable of ligating to an active site cysteine residue. The time dependent nature of irreversible inhibition is investigated by performing the binding assay with and without a pre-incubation of compound and TAK1-TAB1. An increase in potency in the pre-incubated assay suggests the candidate compound could b of 10 nM TAK1-TAB1, 2 nM Eu-anti-his antibody, and 100 nM kinase tracer-236 using a 384-well plate format. Background signal is defined in the absence of TAK1-TAB1 and uninhibited signal is defined in the presence of vehicle (2% DMSO) alone. Compounds were evaluated in an 11 point dose-response ranging from 20 uM to 0.34 nM. The binding assays are performed under two conditions to evaluate time dependence of inhibition. For the pre-incubation assay, TAK1-TAB1 and Eu-anti-his antibody are preincubated with compound or vehicle for two hours prior to the addition of kinase tracer. The non-preincubated assay is run in which TAK1-TAB1 and Eu-anti-his antibody are added to a mixture of compound and kinase tracer. IC50 values of compounds are determined using a 4 parameter logistical fit of emission ratio as a function of the concentration of compound. | 36 | ALA3887013 | single protein format | BindingDB Database |
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