Reaction Details |
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Target | Serine/threonine-protein kinase PLK4 |
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Ligand | BDBM50044666 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1450851 (CHEMBL3364610) |
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IC50 | 3.6±n/a nM |
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Citation | Sampson, PB; Liu, Y; Patel, NK; Feher, M; Forrest, B; Li, SW; Edwards, L; Laufer, R; Lang, Y; Ban, F; Awrey, DE; Mao, G; Plotnikova, O; Leung, G; Hodgson, R; Mason, JM; Wei, X; Kiarash, R; Green, E; Qiu, W; Chirgadze, NY; Mak, TW; Pan, G; Pauls, HW The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. J Med Chem58:130-46 (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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BDBM50044666 |
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n/a |
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Name | BDBM50044666 |
Synonyms: | CHEMBL3353340 | US10358436, Example A22 |
Type | Small organic molecule |
Emp. Form. | C24H18N4O |
Mol. Mass. | 378.4259 |
SMILES | O=C1Nc2ccccc2[C@]11C[C@H]1c1ccc2c(\C=C\c3ccncc3)n[nH]c2c1 |r| |
Structure |
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