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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50458959
Substrate
n/a
Meas. Tech.
ChEMBL_1765178 (CHEMBL4200425)
IC50
37±n/a nM
Citation
 Liu, S; Yosief, HO; Dai, L; Huang, H; Dhawan, G; Zhang, X; Muthengi, AM; Roberts, J; Buckley, DL; Perry, JA; Wu, L; Bradner, JE; Qi, J; Zhang, W Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors. J Med Chem 61:7785-7795 (2018) [PubMed]  Article
Target
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:
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDKYGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS
  
Inhibitor
Name:
BDBM50458959
Synonyms:
CHEMBL4214823
Type:
Small organic molecule
Emp. Form.:
C28H39N7O3
Mol. Mass.:
521.6544
SMILES:
CC[C@H]1N(C2CCCCC2)c2nc(Nc3ccc(cc3OC)C(=O)NC3CCN(C)CC3)ncc2NC1=O |r|
Structure:
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