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TargetSerine/threonine-protein kinase PLK1
LigandBDBM50329917
Substrate/Competitorn/a
Meas. Tech.ChEMBL_675877 (CHEMBL1272694)
IC50 127±n/a nM
Citation Beria, IValsasina, BBrasca, MGCeccarelli, WColombo, MCribioli, SFachin, GFerguson, RDFiorentini, FGianellini, LMGiorgini, MLMoll, JKPosteri, HPezzetta, DRoletto, FSola, FTesei, DCaruso, M 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. Bioorg Med Chem Lett20:6489-94 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase PLK1
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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  Blast E-value cutoff:
BDBM50329917
n/a
NameBDBM50329917
Synonyms:4-(3-(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-ylamino)-4-(trifluoromethoxy)phenyl)-1-methylpiperazine 1-oxide | CHEMBL1271645
TypeSmall organic molecule
Emp. Form.C23H25F3N8O3
Mol. Mass.518.4916
SMILESCn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)N4CC[N+](C)([O-])CC4)nc3-c12
Structure
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