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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM28183
Substrate
PLK Substrate Peptide
Meas. Tech.
Scintillation Proximity Assay (SPA)
IC50
8±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
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:
Human
Description:
P53350
Residue:
603
Sequence:
MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLGKGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFFEDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLGNLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCIMYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELLNDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEEPVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDKYGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLKYFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTKLILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRLKAS
Inhibitor
Name:
BDBM28183
Synonyms:
5-(5,6-dimethoxy-1H-1,3-benzodiazol-1-yl)-3-[(2-methoxyphenyl)methoxy]thiophene-2-carboxamide | benzimidazole thiophene analogue, 34
Type:
Small organic molecule
Emp. Form.:
C22H21N3O5S
Mol. Mass.:
439.484
SMILES:
COc1ccccc1COc1cc(sc1C(N)=O)-n1cnc2cc(OC)c(OC)cc12
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