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TargetSerine/threonine-protein kinase PLK4
LigandBDBM50073582
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1467184 (CHEMBL3411381)
IC50 1.4±n/a nM
Citation Sampson, PBLiu, YForrest, BCumming, GLi, SWPatel, NKEdwards, LLaufer, RFeher, MBan, FAwrey, DEMao, GPlotnikova, OHodgson, RBeletskaya, IMason, JMLuo, XNadeem, VWei, XKiarash, RMadeira, BHuang, PMak, TWPan, GPauls, 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
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase PLK4
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50073582
n/a
NameBDBM50073582
Synonyms:CHEMBL3408942 | US10358436, Example A109 | US9907800, Example A109
TypeSmall organic molecule
Emp. Form.C29H28N4O
Mol. Mass.448.5588
SMILESCN(C)Cc1ccc(\C=C\c2n[nH]c3cc(ccc23)[C@@H]2C[C@@]22C(=O)N(C)c3ccccc23)cc1 |r|
Structure
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