Reaction Details |
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Target | Serine/threonine-protein kinase PLK4 |
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Ligand | BDBM50044675 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1467184 (CHEMBL3411381) |
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IC50 | 1.4±n/a nM |
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Citation | Sampson, PB; Liu, Y; Forrest, B; Cumming, G; Li, SW; Patel, NK; Edwards, L; Laufer, R; Feher, M; Ban, F; Awrey, DE; Mao, G; Plotnikova, O; Hodgson, R; Beletskaya, I; Mason, JM; Luo, X; Nadeem, V; Wei, X; Kiarash, R; Madeira, B; Huang, P; Mak, TW; Pan, G; Pauls, HW The discovery of Polo-like kinase 4 inhibitors: identification of (1R,2S).2-(3-((E).4-(((cis).2,6-dimethylmorpholino)methyl)styryl). 1H.indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one (CFI-400945) as a potent, orally active antitumor agent. J Med Chem58:147-69 (2015) [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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BDBM50044675 |
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n/a |
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Name | BDBM50044675 |
Synonyms: | CHEMBL3353354 | US10358436, Example A56 | US9907800, Example A56 |
Type | Small organic molecule |
Emp. Form. | C30H28N4O2 |
Mol. Mass. | 476.5689 |
SMILES | O=C1Nc2ccccc2[C@]11C[C@H]1c1ccc2c(\C=C\c3ccc(CN4CCOCC4)cc3)n[nH]c2c1 |r| |
Structure |
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