Reaction Details |
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Target | Serine/threonine-protein kinase PLK1 |
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Ligand | BDBM25121 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1728206 (CHEMBL4143484) |
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IC50 | 5.3±n/a nM |
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Citation | Zhan, MM; Yang, Y; Luo, J; Zhang, XX; Xiao, X; Li, S; Cheng, K; Xie, Z; Tu, Z; Liao, C Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold. Eur J Med Chem143:724-731 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Serine/threonine-protein kinase PLK1 |
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Name: | Serine/threonine-protein kinase PLK1 |
Synonyms: | PLK | PLK-1 | PLK1 | PLK1_HUMAN | Polo-like kinase 1 (PlK1) | Polo-like kinase 1 (Plk-1) | STPK13 | Serine/threonine-protein kinase (PLK1) | Serine/threonine-protein kinase 13 | polo-like kinase |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 68277.16 |
Organism: | Homo sapiens (Human) |
Description: | P53350 |
Residue: | 603 |
Sequence: | MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLG
KGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFF
EDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLG
NLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCI
MYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELL
NDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEE
PVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDK
YGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLK
YFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTK
LILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRL
KAS
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BDBM25121 |
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n/a |
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Name | BDBM25121 |
Synonyms: | 4-{[(7R)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | BI 2536 | CHEMBL513909 | US10450297, Example 300 | US8598172, 5 |
Type | Small organic molecule |
Emp. Form. | C28H39N7O3 |
Mol. Mass. | 521.6544 |
SMILES | CC[C@H]1N(C2CCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCN(C)CC3)ncc2N(C)C1=O |r| |
Structure |
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