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Target
Serine/threonine-protein kinase PLK4
Ligand
BDBM375291
Substrate
n/a
Meas. Tech.
ChEMBL_1927292 (CHEMBL4430364)
IC50
1.000000±n/a nM
Citation
 Li, SW; Liu, Y; Sampson, PB; Patel, NK; Forrest, BT; Edwards, L; Laufer, R; Feher, M; Ban, F; Awrey, DE; Hodgson, R; Beletskaya, I; Mao, G; Mason, JM; Wei, X; Luo, X; Kiarash, R; Green, E; Mak, TW; Pan, G; Pauls, 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 Lett 26:4625-4630 (2016) [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:
BDBM375291
Synonyms:
US10358436, Example A16 | US9907800, Example A16
Type:
Small organic molecule
Emp. Form.:
C28H28N6O2
Mol. Mass.:
480.5609
SMILES:
COc1ccc2NC(=O)[C@@]3(C[C@H]3c3ccc4c(n[nH]c4c3)-c3ccc(nc3)N3CCN(C)CC3)c2c1 |r|
Structure:
Search PDB for entries with ligand similarity: