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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM50044657
Substrate
n/a
Meas. Tech.
ChEMBL_1450867 (CHEMBL3364626)
IC50
>100000±n/a nM
Citation
 Sampson, PB; Liu, Y; Patel, NK; Feher, M; Forrest, B; Li, SW; Edwards, L; Laufer, R; Lang, Y; Ban, F; Awrey, DE; Mao, G; Plotnikova, O; Leung, G; Hodgson, R; Mason, JM; Wei, X; Kiarash, R; Green, E; Qiu, W; Chirgadze, NY; Mak, TW; Pan, G; Pauls, HW The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. J Med Chem 58:130-46 (2015) [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:
BDBM50044657
Synonyms:
CHEMBL3353347 | US10358436, Example A24 | US9907800, Example A24
Type:
Small organic molecule
Emp. Form.:
C28H26N4O
Mol. Mass.:
434.5322
SMILES:
CN(C)Cc1ccc(\C=C\c2n[nH]c3cc(ccc23)[C@@H]2C[C@@]22C(=O)Nc3ccccc23)cc1 |r|
Structure:
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