Reaction Details |
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Target | MAP kinase-activated protein kinase 5 |
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Ligand | BDBM50308060 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_655455 (CHEMBL1244499) |
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Kd | 930±n/a nM |
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Citation | Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood114:2984-92 (2009) [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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BDBM50308060 |
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n/a |
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Name | BDBM50308060 |
Synonyms: | 16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one | CEP-701 | CHEMBL603469 | US11370779, Compound CEP-701 |
Type | Small organic molecule |
Emp. Form. | C26H21N3O4 |
Mol. Mass. | 439.4626 |
SMILES | C[C@]12O[C@H](C[C@]1(O)CO)n1c3ccccc3c3c4C(=O)NCc4c4c5ccccc5n2c4c13 |r| |
Structure |
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