Reaction Details |
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Target | MAP kinase-activated protein kinase 5 |
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Ligand | BDBM50355393 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_773486 (CHEMBL1839852) |
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IC50 | >10000±n/a nM |
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Citation | Guagnano, V; Furet, P; Spanka, C; Bordas, V; Le Douget, M; Stamm, C; Brueggen, J; Jensen, MR; Schnell, C; Schmid, H; Wartmann, M; Berghausen, J; Drueckes, P; Zimmerlin, A; Bussiere, D; Murray, J; Graus Porta, D Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem54:7066-83 (2011) [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 5 |
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Name: | MAP kinase-activated protein kinase 5 |
Synonyms: | MAP kinase-activated protein kinase 5 (PRAK) | MAPK-Activated Protein Kinase 5 (MK5) | MAPK-activated protein kinase 5 | MAPK5_HUMAN | MAPKAP kinase 5 | MAPKAPK5 | PRAK | p38-regulated/activated protein kinase | p38-regulated/activated protein kinase (PRAK) |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 54229.92 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant MAPKAPK5 was phosphorylated by incubation with active p38alpha before assays. |
Residue: | 473 |
Sequence: | MSEESDMDKAIKETSILEEYSINWTQKLGAGISGPVRVCVKKSTQERFALKILLDRPKAR
NEVRLHMMCATHPNIVQIIEVFANSVQFPHESSPRARLLIVMEMMEGGELFHRISQHRHF
TEKQASQVTKQIALALRHCHLLNIAHRDLKPENLLFKDNSLDAPVKLCDFGFAKIDQGDL
MTPQFTPYYVAPQVLEAQRRHQKEKSGIIPTSPTPYTYNKSCDLWSLGVIIYVMLCGYPP
FYSKHHSRTIPKDMRRKIMTGSFEFPEEEWSQISEMAKDVVRKLLKVKPEERLTIEGVLD
HPWLNSTEALDNVLPSAQLMMDKAVVAGIQQAHAEQLANMRIQDLKVSLKPLHSVNNPIL
RKRKLLGTKPKDSVYIHDHENGAEDSNVALEKLRDVIAQCILPQAGKGENEDEKLNEVMQ
EAWKYNRECKLLRDTLQSFSWNGRGFTDKVDRLKLAEIVKQVIEEQTTSHESQ
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BDBM50355393 |
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n/a |
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Name | BDBM50355393 |
Synonyms: | BGJ398 | CHEMBL1834657 | US9434697, BGJ398 | US9730931, BGJ398 |
Type | Small organic molecule |
Emp. Form. | C26H31Cl2N7O3 |
Mol. Mass. | 560.475 |
SMILES | CCN1CCN(CC1)c1ccc(Nc2cc(ncn2)N(C)C(=O)Nc2c(Cl)c(OC)cc(OC)c2Cl)cc1 |
Structure |
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