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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50343561
Substrate
n/a
Meas. Tech.
ChEMBL_747145 (CHEMBL1777511)
IC50
43±n/a nM
Citation
 Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Re Depaolini, S; Valsasina, 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 Lett 21:2969-74 (2011) [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:
BDBM50343561
Synonyms:
8-(5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-1-(2-(tetrahydro-2H-pyran-4-yloxy)ethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774338
Type:
Small organic molecule
Emp. Form.:
C29H35F3N8O4
Mol. Mass.:
616.6346
SMILES:
CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCOC5CCOCC5)c4-c3n2)C(N)=O)c1
Structure:
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