Target
Serine/threonine-protein kinase PLK4
Ligand
BDBM50591963
Substrate
n/a
Meas. Tech.
ChEMBL_2202882 (CHEMBL5115590)
IC50
22±n/a nM
Citation
 Sun, YSun, YWang, LWu, TYin, WWang, JXue, YQin, QSun, YYang, HZhao, DCheng, 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]  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:
BDBM50591963
Synonyms:
CHEMBL5173724
Type:
Small organic molecule
Emp. Form.:
C24H24N6O
Mol. Mass.:
412.487
SMILES:
CN(C)Cc1ccc(\C=C\c2n[nH]c3cc(ccc23)-c2ccnc(NC(C)=O)n2)cc1
Structure:
Search PDB for entries with ligand similarity: