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TargetSerine/threonine-protein kinase PLK1
LigandBDBM50329926
Substrate/Competitorn/a
Meas. Tech.ChEMBL_675877 (CHEMBL1272694)
IC50 4±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:
BDBM50329926
n/a
NameBDBM50329926
Synonyms:8-(5-(piperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1271695
TypeSmall organic molecule
Emp. Form.C22H23F3N8O2
Mol. Mass.488.4656
SMILESCN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(n[nH]c4C(N)=O)-c3n2)c1
Structure
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