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TargetSerine/threonine-protein kinase PLK1
LigandBDBM50343565
Substrate/Competitorn/a
Meas. Tech.ChEMBL_747145 (CHEMBL1777511)
IC50 83±n/a nM
Citation Beria, IBossi, RTBrasca, MGCaruso, MCeccarelli, WFachin, GFasolini, MForte, BFiorentini, FPesenti, EPezzetta, DPosteri, HScolaro, ARe Depaolini, SValsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett21:2969-74 (2011) [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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BDBM50343565
n/a
NameBDBM50343565
Synonyms:1-methyl-8-(5-(pyrrolidin-2-ylamino)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774332
TypeSmall organic molecule
Emp. Form.C22H23F3N8O2
Mol. Mass.488.4656
SMILESCn1nc(C(N)=O)c2CCc3cnc(Nc4cc(NC5CCCN5)ccc4OC(F)(F)F)nc3-c12
Structure
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