Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50318088
Substrate
n/a
Meas. Tech.
ChEMBL_631389 (CHEMBL1109141)
IC50
100±n/a nM
Citation
 Beria, IBallinari, DBertrand, JABorghi, DBossi, RTBrasca, MGCappella, PCaruso, MCeccarelli, WCiavolella, ACristiani, CCroci, VDe Ponti, AFachin, GFerguson, RDLansen, JMoll, JKPesenti, EPosteri, HPerego, RRocchetti, MStorici, PVolpi, DValsasina, B Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J Med Chem 53:3532-51 (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:
Homo sapiens (Human)
Description:
P53350
Residue:
603
Sequence:
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDKYGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS
  
Inhibitor
Name:
BDBM50318088
Synonyms:
8-[(3-Acetylphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | CHEMBL1099105
Type:
Small organic molecule
Emp. Form.:
C19H18N6O2
Mol. Mass.:
362.3852
SMILES:
CC(=O)c1cccc(Nc2ncc3CCc4c(nn(C)c4-c3n2)C(N)=O)c1
Structure:
Search PDB for entries with ligand similarity: