Reaction Details Report a problem with these data
Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50329916
Substrate
n/a
Meas. Tech.
ChEMBL_675877 (CHEMBL1272694)
IC50
7±n/a nM
Citation
 Beria, I; Valsasina, B; Brasca, MG; Ceccarelli, W; Colombo, M; Cribioli, S; Fachin, G; Ferguson, RD; Fiorentini, F; Gianellini, LM; Giorgini, ML; Moll, JK; Posteri, H; Pezzetta, D; Roletto, F; Sola, F; Tesei, D; Caruso, M 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. Bioorg Med Chem Lett 20:6489-94 (2010) [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:
Human
Description:
P53350
Residue:
603
Sequence:
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDKYGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS
  
Inhibitor
Name:
BDBM50329916
Synonyms:
1-(2-chloroethyl)-8-(5-(piperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1271869
Type:
Small organic molecule
Emp. Form.:
C24H26ClF3N8O2
Mol. Mass.:
550.964
SMILES:
CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(CCCl)c4-c3n2)C(N)=O)c1
Structure:
Search PDB for entries with ligand similarity: