Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM27452
Substrate
PLK1 Substrate Peptide
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
794±n/a nM
Citation
 Bamborough, PChristopher, JACutler, GJDickson, MCMellor, GWMorey, JVPatel, CBShewchuk, LM 5-(1H-Benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-epsilon kinase. Bioorg Med Chem Lett 16:6236-40 (2006) [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:
BDBM27452
Synonyms:
5-(5,6-dimethoxy-1H-1,3-benzodiazol-1-yl)-3-[(2-methanesulfonylphenyl)methoxy]thiophene-2-carbonitrile | benzimidazole-thiophene carbonitrile, 12e
Type:
Small organic molecule
Emp. Form.:
C22H19N3O5S2
Mol. Mass.:
469.533
SMILES:
COc1cc2ncn(-c3cc(OCc4ccccc4S(C)(=O)=O)c(s3)C#N)c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PLK1 Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1720.29
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINAHSFNDTLDFD