Ki Summary BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetSerine/threonine-protein kinase PLK4
LigandBDBM25117
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1450851 (CHEMBL3364610)
IC50 43±n/a nM
Citation Sampson, PBLiu, YPatel, NKFeher, MForrest, BLi, SWEdwards, LLaufer, RLang, YBan, FAwrey, DEMao, GPlotnikova, OLeung, GHodgson, RMason, JMWei, XKiarash, RGreen, EQiu, WChirgadze, NYMak, TWPan, GPauls, HW The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. J Med Chem58:130-46 (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:
BDBM25117
n/a
NameBDBM25117
Synonyms:AG-013736 | AXITINIB | N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide | US10464902, Axitinib | US9205078, Axitinib | US9617222, Compound A
TypeSmall organic molecule
Emp. Form.C22H18N4OS
Mol. Mass.386.47
SMILESCNC(=O)c1ccccc1Sc1ccc2c(\C=C\c3ccccn3)n[nH]c2c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: