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Target
Serine/threonine-protein kinase PLK1
Ligand
BDBM25520
Substrate
Cdc25C Substrate Peptide
Meas. Tech.
Plk in Vitro Assay
pH
7.2±n/a
Temperature
303.15±n/a K
IC50
59±n/a nM
Citation
Fucini, RV; Hanan, EJ; Romanowski, MJ; Elling, RA; Lew, W; Barr, KJ; Zhu, J; Yoburn, JC; Liu, Y; Fahr, BT; Fan, J; Lu, Y; Pham, P; Choong, IC; VanderPorten, EC; Bui, M; Purkey, HE; Evanchik, MJ; Yang, W Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors. Bioorg Med Chem Lett 18:5648-52 (2008) [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:
BDBM25520
Synonyms:
1-[3-(3-aminopropyl)-5-chlorophenyl]-3-methyl-N-[(1S)-1-phenylethyl]-1H-pyrazolo[4,3-c]pyridin-6-amine | 2-amino-pyrazolopyridine, 36
Type:
Small organic molecule
Emp. Form.:
C24H26ClN5
Mol. Mass.:
419.95
SMILES:
C[C@H](Nc1cc2n(nc(C)c2cn1)-c1cc(Cl)cc(CCCN)c1)c1ccccc1 |r|
Substrate
Name:
Cdc25C Substrate Peptide
Synonyms:
5-carboxamido-fluorescein (5FAM) labeled peptide
Type:
Fluorophore tagged peptide
Mol. Mass.:
2066.83
Organism:
n/a
Description:
n/a
Residue:
18
Sequence:
FAMRALMEASFADQARNH