Reaction Details Report a problem with these data
Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM28201
Substrate
PLK Substrate Peptide
Meas. Tech.
Scintillation Proximity Assay (SPA)
IC50
73±n/a nM
Citation
 Emmitte, KA; Andrews, CW; Badiang, JG; Davis-Ward, RG; Dickson, HD; Drewry, DH; Emerson, HK; Epperly, AH; Hassler, DF; Knick, VB; Kuntz, KW; Lansing, TJ; Linn, JA; Mook, RA; Nailor, KE; Salovich, JM; Spehar, GM; Cheung, M Discovery of thiophene inhibitors of polo-like kinase. Bioorg Med Chem Lett 19:1018-21 (2009) [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:
BDBM28201
Synonyms:
5,6-dimethoxy-1-[5-(1H-1,2,3,4-tetrazol-5-yl)-4-{[2-(trifluoromethyl)phenyl]methoxy}thiophen-2-yl]-1H-1,3-benzodiazole | benzimidazole thiophene analogue, 54
Type:
Small organic molecule
Emp. Form.:
C22H17F3N6O3S
Mol. Mass.:
502.469
SMILES:
COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)-c3nnn[nH]3)c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PLK Substrate Peptide
Synonyms:
n/a
Type:
Biotinylated peptide
Mol. Mass.:
1720.29
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINAHSFNDTLDFD