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Target
Serine/threonine-protein kinase PLK4
Ligand
BDBM50004205
Substrate
n/a
Meas. Tech.
ChEMBL_2202874 (CHEMBL5115582)
Ki
7.7±n/a nM
Citation
 Sun, Y; Sun, Y; Wang, L; Wu, T; Yin, W; Wang, J; Xue, Y; Qin, Q; Sun, Y; Yang, H; Zhao, D; Cheng, M Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer. Eur J Med Chem 238:0 (2022) [PubMed] 
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:
BDBM50004205
Synonyms:
MK-045 | MK-0457 | TOZASERTIB | US9249124, VX680 | VX-68 | VX-680
Type:
Small organic molecule
Emp. Form.:
C23H28N8OS
Mol. Mass.:
464.586
SMILES:
CN1CCN(CC1)c1cc(Nc2cc(C)[nH]n2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1
Structure:
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