Reaction Details |
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Target | Serine/threonine-protein kinase PLK4 |
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Ligand | BDBM50533815 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1927292 (CHEMBL4430364) |
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IC50 | 2.4±n/a nM |
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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 Lett26:4625-4630 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase PLK4 |
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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
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BDBM50533815 |
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n/a |
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Name | BDBM50533815 |
Synonyms: | CHEMBL4434704 |
Type | Small organic molecule |
Emp. Form. | C27H26N6O2 |
Mol. Mass. | 466.5343 |
SMILES | COc1ccc2NC(=O)C(=Cc3ccc4c(n[nH]c4c3)-c3ccc(nc3)N3CCN(C)CC3)c2c1 |
Structure |
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