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TargetSerine/threonine-protein kinase PLK4
LigandBDBM50533815
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1927292 (CHEMBL4430364)
IC50 2.4±n/a nM
Citation Li, SWLiu, YSampson, PBPatel, NKForrest, BTEdwards, LLaufer, RFeher, MBan, FAwrey, DEHodgson, RBeletskaya, IMao, GMason, JMWei, XLuo, XKiarash, RGreen, EMak, TWPan, GPauls, HW Design and optimization of (3-aryl-1H-indazol-6-yl)spiro[cyclopropane-1,3'-indolin]-2'-ones as potent PLK4 inhibitors with oral antitumor efficacy. Bioorg Med Chem Lett26:4625-4630 (2016) [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:
BDBM50533815
n/a
NameBDBM50533815
Synonyms:CHEMBL4434704
TypeSmall organic molecule
Emp. Form.C27H26N6O2
Mol. Mass.466.5343
SMILESCOc1ccc2NC(=O)C(=Cc3ccc4c(n[nH]c4c3)-c3ccc(nc3)N3CCN(C)CC3)c2c1
Structure
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