Reaction Details |
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Target | Serine/threonine-protein kinase PLK4 |
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Ligand | BDBM50081537 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1474078 (CHEMBL3423973) |
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IC50 | 130±n/a nM |
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Citation | Liu, Y; Lang, Y; Patel, NK; Ng, G; Laufer, R; Li, SW; Edwards, L; Forrest, B; Sampson, PB; Feher, M; Ban, F; Awrey, DE; Beletskaya, I; Mao, G; Hodgson, R; Plotnikova, O; Qiu, W; Chirgadze, NY; Mason, JM; Wei, X; Lin, DC; Che, Y; Kiarash, R; Madeira, B; Fletcher, GC; Mak, TW; Bray, MR; Pauls, HW The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as Anticancer Agents. J Med Chem58:3366-92 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase PLK4 |
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Name: | Serine/threonine-protein kinase PLK4 |
Synonyms: | PLK4 | PLK4_HUMAN | Polo-Like Kinase 4 | SAK | STK18 | Serine/threonine-protein kinase PLK4 |
Type: | PROTEIN |
Mol. Mass.: | 108996.91 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_1474078 |
Residue: | 970 |
Sequence: | MATCIGEKIEDFKVGNLLGKGSFAGVYRAESIHTGLEVAIKMIDKKAMYKAGMVQRVQNE
VKIHCQLKHPSILELYNYFEDSNYVYLVLEMCHNGEMNRYLKNRVKPFSENEARHFMHQI
ITGMLYLHSHGILHRDLTLSNLLLTRNMNIKIADFGLATQLKMPHEKHYTLCGTPNYISP
EIATRSAHGLESDVWSLGCMFYTLLIGRPPFDTDTVKNTLNKVVLADYEMPSFLSIEAKD
LIHQLLRRNPADRLSLSSVLDHPFMSRNSSTKSKDLGTVEDSIDSGHATISTAITASSST
SISGSLFDKRRLLIGQPLPNKMTVFPKNKSSTDFSSSGDGNSFYTQWGNQETSNSGRGRV
IQDAEERPHSRYLRRAYSSDRSGTSNSQSQAKTYTMERCHSAEMLSVSKRSGGGENEERY
SPTDNNANIFNFFKEKTSSSSGSFERPDNNQALSNHLCPGKTPFPFADPTPQTETVQQWF
GNLQINAHLRKTTEYDSISPNRDFQGHPDLQKDTSKNAWTDTKVKKNSDASDNAHSVKQQ
NTMKYMTALHSKPEIIQQECVFGSDPLSEQSKTRGMEPPWGYQNRTLRSITSPLVAHRLK
PIRQKTKKAVVSILDSEEVCVELVKEYASQEYVKEVLQISSDGNTITIYYPNGGRGFPLA
DRPPSPTDNISRYSFDNLPEKYWRKYQYASRFVQLVRSKSPKITYFTRYAKCILMENSPG
ADFEVWFYDGVKIHKTEDFIQVIEKTGKSYTLKSESEVNSLKEEIKMYMDHANEGHRICL
ALESIISEEERKTRSAPFFPIIIGRKPGSTSSPKALSPPPSVDSNYPTRERASFNRMVMH
SAASPTQAPILNPSMVTNEGLGLTTTASGTDISSNSLKDCLPKSAQLLKSVFVKNVGWAT
QLTSGAVWVQFNDGSQLVVQAGVSSISYTSPNGQTTRYGENEKLPDYIKQKLQCLSSILL
MFSNPTPNFH
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BDBM50081537 |
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n/a |
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Name | BDBM50081537 |
Synonyms: | CHEMBL3422092 |
Type | Small organic molecule |
Emp. Form. | C30H31N5O2 |
Mol. Mass. | 493.5994 |
SMILES | [H][C@]12CC[C@@]([H])(CC(O)C1)N2c1ccc(cc1)-c1n[nH]c2ccc(cc12)C(=O)N[C@H](C1CC1)c1ccccn1 |r,@:7| |
Structure |
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