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Target
Serine/threonine-protein kinase PLK4
Ligand
BDBM25117
Substrate
n/a
Meas. Tech.
ChEMBL_973993 (CHEMBL2410318)
IC50
46±n/a nM
Citation
 Laufer, R; Forrest, B; Li, SW; Liu, Y; Sampson, P; Edwards, L; Lang, Y; Awrey, DE; Mao, G; Plotnikova, O; Leung, G; Hodgson, R; Beletskaya, I; Mason, JM; Luo, X; Wei, X; Yao, Y; Feher, M; Ban, F; Kiarash, R; Green, E; Mak, TW; Pan, G; Pauls, HW The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem 56:6069-87 (2013) [PubMed]  Article 
Target
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:
MATCIGEKIEDFKVGNLLGKGSFAGVYRAESIHTGLEVAIKMIDKKAMYKAGMVQRVQNEVKIHCQLKHPSILELYNYFEDSNYVYLVLEMCHNGEMNRYLKNRVKPFSENEARHFMHQIITGMLYLHSHGILHRDLTLSNLLLTRNMNIKIADFGLATQLKMPHEKHYTLCGTPNYISPEIATRSAHGLESDVWSLGCMFYTLLIGRPPFDTDTVKNTLNKVVLADYEMPSFLSIEAKDLIHQLLRRNPADRLSLSSVLDHPFMSRNSSTKSKDLGTVEDSIDSGHATISTAITASSSTSISGSLFDKRRLLIGQPLPNKMTVFPKNKSSTDFSSSGDGNSFYTQWGNQETSNSGRGRVIQDAEERPHSRYLRRAYSSDRSGTSNSQSQAKTYTMERCHSAEMLSVSKRSGGGENEERYSPTDNNANIFNFFKEKTSSSSGSFERPDNNQALSNHLCPGKTPFPFADPTPQTETVQQWFGNLQINAHLRKTTEYDSISPNRDFQGHPDLQKDTSKNAWTDTKVKKNSDASDNAHSVKQQNTMKYMTALHSKPEIIQQECVFGSDPLSEQSKTRGMEPPWGYQNRTLRSITSPLVAHRLKPIRQKTKKAVVSILDSEEVCVELVKEYASQEYVKEVLQISSDGNTITIYYPNGGRGFPLADRPPSPTDNISRYSFDNLPEKYWRKYQYASRFVQLVRSKSPKITYFTRYAKCILMENSPGADFEVWFYDGVKIHKTEDFIQVIEKTGKSYTLKSESEVNSLKEEIKMYMDHANEGHRICLALESIISEEERKTRSAPFFPIIIGRKPGSTSSPKALSPPPSVDSNYPTRERASFNRMVMHSAASPTQAPILNPSMVTNEGLGLTTTASGTDISSNSLKDCLPKSAQLLKSVFVKNVGWATQLTSGAVWVQFNDGSQLVVQAGVSSISYTSPNGQTTRYGENEKLPDYIKQKLQCLSSILLMFSNPTPNFH
  
Inhibitor
Name:
BDBM25117
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
Type:
Small organic molecule
Emp. Form.:
C22H18N4OS
Mol. Mass.:
386.47
SMILES:
CNC(=O)c1ccccc1Sc1ccc2c(\C=C\c3ccccn3)n[nH]c2c1
Structure:
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