Reaction Details |
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Target | Dual specificity protein kinase TTK |
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Ligand | BDBM50183029 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1586153 (CHEMBL3821249) |
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IC50 | 32±n/a nM |
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Citation | Laufer, R; Li, SW; Liu, Y; Ng, G; Lang, Y; Feher, M; Brokx, R; Beletskaya, I; Hodgson, R; Mao, G; Plotnikova, O; Awrey, DE; Mason, JM; Wei, X; Lin, DC; Che, Y; Kiarash, R; Madeira, B; Fletcher, GC; Mak, TW; Bray, MR; Pauls, HW Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK. Bioorg Med Chem Lett26:3562-6 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity protein kinase TTK |
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Name: | Dual specificity protein kinase TTK |
Synonyms: | Dual specificity protein kinase (TTK) | Dual specificity protein kinase TTK (MPS1) | MPS1 | MPS1L1 | Monopolar Spindle 1 (MPS1) | Monopolar Spindle 1 (Mps-1) | Monopolar Spindle 1 Kinase (MPS1) | Phosphotyrosine picked threonine-protein kinase (MPS1) | TTK | TTK_HUMAN |
Type: | Protein |
Mol. Mass.: | 97086.79 |
Organism: | Homo sapiens (Human) |
Description: | P33981 |
Residue: | 857 |
Sequence: | MESEDLSGRELTIDSIMNKVRDIKNKFKNEDLTDELSLNKISADTTDNSGTVNQIMMMAN
NPEDWLSLLLKLEKNSVPLSDALLNKLIGRYSQAIEALPPDKYGQNESFARIQVRFAELK
AIQEPDDARDYFQMARANCKKFAFVHISFAQFELSQGNVKKSKQLLQKAVERGAVPLEML
EIALRNLNLQKKQLLSEEEKKNLSASTVLTAQESFSGSLGHLQNRNNSCDSRGQTTKARF
LYGENMPPQDAEIGYRNSLRQTNKTKQSCPFGRVPVNLLNSPDCDVKTDDSVVPCFMKRQ
TSRSECRDLVVPGSKPSGNDSCELRNLKSVQNSHFKEPLVSDEKSSELIITDSITLKNKT
ESSLLAKLEETKEYQEPEVPESNQKQWQSKRKSECINQNPAASSNHWQIPELARKVNTEQ
KHTTFEQPVFSVSKQSPPISTSKWFDPKSICKTPSSNTLDDYMSCFRTPVVKNDFPPACQ
LSTPYGQPACFQQQQHQILATPLQNLQVLASSSANECISVKGRIYSILKQIGSGGSSKVF
QVLNEKKQIYAIKYVNLEEADNQTLDSYRNEIAYLNKLQQHSDKIIRLYDYEITDQYIYM
VMECGNIDLNSWLKKKKSIDPWERKSYWKNMLEAVHTIHQHGIVHSDLKPANFLIVDGML
KLIDFGIANQMQPDTTSVVKDSQVGTVNYMPPEAIKDMSSSRENGKSKSKISPKSDVWSL
GCILYYMTYGKTPFQQIINQISKLHAIIDPNHEIEFPDIPEKDLQDVLKCCLKRDPKQRI
SIPELLAHPYVQIQTHPVNQMAKGTTEEMKYVLGQLVGLNSPNSILKAAKTLYEHYSGGE
SHNSSSSKTFEKKRGKK
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BDBM50183029 |
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n/a |
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Name | BDBM50183029 |
Synonyms: | CHEMBL3818025 |
Type | Small organic molecule |
Emp. Form. | C26H32ClN7O3 |
Mol. Mass. | 526.03 |
SMILES | Clc1cc(ccc1C(=O)NC1CC1)-c1cnn2c(NCC3CCOCC3)nc(NC3CCOCC3)nc12 |
Structure |
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