Reaction Details |
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Target | MAP kinase-activated protein kinase 3 |
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Ligand | BDBM50401152 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_881231 (CHEMBL2211536) |
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IC50 | <10000±n/a nM |
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Citation | Sunose, M; Bell, K; Ellard, K; Bergamini, G; Neubauer, G; Werner, T; Ramsden, N Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. Bioorg Med Chem Lett22:4613-8 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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MAP kinase-activated protein kinase 3 |
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Name: | MAP kinase-activated protein kinase 3 |
Synonyms: | 3pK | Chromosome 3p kinase | MAP kinase-activated protein kinase 3 (MAPKAP-K3) | MAPK-Activated Protein Kinase 3 (MK3) | MAPK-activated protein kinase 3 | MAPK3_HUMAN | MAPKAP kinase 3 | MAPKAPK-3 | MAPKAPK3 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 42991.57 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant MAPKAPK3 was phosphorylated by incubation with active p38alpha before assays. |
Residue: | 382 |
Sequence: | MDGETAEEQGGPVPPPVAPGGPGLGGAPGGRREPKKYAVTDDYQLSKQVLGLGVNGKVLE
CFHRRTGQKCALKLLYDSPKARQEVDHHWQASGGPHIVCILDVYENMHHGKRCLLIIMEC
MEGGELFSRIQERGDQAFTEREAAEIMRDIGTAIQFLHSHNIAHRDVKPENLLYTSKEKD
AVLKLTDFGFAKETTQNALQTPCYTPYYVAPEVLGPEKYDKSCDMWSLGVIMYILLCGFP
PFYSNTGQAISPGMKRRIRLGQYGFPNPEWSEVSEDAKQLIRLLLKTDPTERLTITQFMN
HPWINQSMVVPQTPLHTARVLQEDKDHWDEVKEEMTSALATMRVDYDQVKIKDLKTSNNR
LLNKRRKKQAGSSSASQGCNNQ
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BDBM50401152 |
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n/a |
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Name | BDBM50401152 |
Synonyms: | CHEMBL2205766 |
Type | Small organic molecule |
Emp. Form. | C15H18N6O2S |
Mol. Mass. | 346.407 |
SMILES | CC(C)(C)NS(=O)(=O)c1cncc(c1)-c1ccn2nc(N)nc2c1 |
Structure |
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