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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50339799
Substrate
n/a
Meas. Tech.
ChEMBL_735641 (CHEMBL1693343)
IC50
190±n/a nM
Citation
Solanki, S; Innocenti, P; Mas-Droux, C; Boxall, K; Barillari, C; van Montfort, RL; Aherne, GW; Bayliss, R; Hoelder, S Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship. J Med Chem 54:1626-39 (2011) [PubMed] Article
More Info.:
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:
BDBM50339799
Synonyms:
(+/-)-4-(6-(1-Methylpiperidin-4-yloxy)-1H-benzo[d]imidazol-1-yl)-2-(1-(2-(trifluoromethyl)phenyl)ethoxy)benzamide | CHEMBL1689164
Type:
Small organic molecule
Emp. Form.:
C29H29F3N4O3
Mol. Mass.:
538.5608
SMILES:
CC(Oc1cc(ccc1C(N)=O)-n1cnc2ccc(OC3CCN(C)CC3)cc12)c1ccccc1C(F)(F)F