Reaction Details |
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Target | Serine/threonine-protein kinase PLK4 |
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Ligand | BDBM50073583 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1467184 (CHEMBL3411381) |
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IC50 | 3.8±n/a nM |
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Citation | Sampson, PB; Liu, Y; Forrest, B; Cumming, G; Li, SW; Patel, NK; Edwards, L; Laufer, R; Feher, M; Ban, F; Awrey, DE; Mao, G; Plotnikova, O; Hodgson, R; Beletskaya, I; Mason, JM; Luo, X; Nadeem, V; Wei, X; Kiarash, R; Madeira, B; Huang, P; Mak, TW; Pan, G; Pauls, HW The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. J Med Chem58:147-69 (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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BDBM50073583 |
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n/a |
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Name | BDBM50073583 |
Synonyms: | CHEMBL3408943 | US9907800, Example A106 |
Type | Small organic molecule |
Emp. Form. | C30H27FN4O |
Mol. Mass. | 478.56 |
SMILES | F[C@@H]1CCN(Cc2ccc(\C=C\c3n[nH]c4cc(ccc34)[C@@H]3C[C@@]33C(=O)Nc4ccccc34)cc2)C1 |r| |
Structure |
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