Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM50362981
Substrate
n/a
Meas. Tech.
ChEMBL_800413 (CHEMBL1948344)
IC50
18±n/a nM
Citation
 Duffey, MOVos, TJAdams, RAlley, JAnthony, JBarrett, CBharathan, IBowman, DBump, NJChau, RCullis, CDriscoll, DLElder, AForsyth, NFrazer, JGuo, JGuo, LHyer, MLJanowick, DKulkarni, BLai, SJLasky, KLi, GLi, JLiao, DLittle, JPeng, BQian, MGReynolds, DJRezaei, MScott, MPSells, TBShinde, VShi, QJSintchak, MDSoucy, FSprott, KTStroud, SGNestor, MVisiers, IWeatherhead, GYe, YD'Amore, N Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). J Med Chem 55:197-208 (2012) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase PLK3
Synonyms:
CNK | Cytokine-inducible serine/threonine-protein kinase | FGF-inducible kinase | FNK | PLK3 | PLK3_HUMAN | PRK | Polo-Like Kinase 3 | Proliferation-related kinase | Serine/threonine-protein kinase PLK3
Type:
Serine/threonine-protein kinase
Mol. Mass.:
71655.17
Organism:
Homo sapiens (Human)
Description:
Enzyme assays were using PLK3 purified from baculovirus-infected Trichoplusia ni cells expressing full-length PLK3.
Residue:
646
Sequence:
MEPAAGFLSPRPFQRAAAAPAPPAGPGPPPSALRGPELEMLAGLPTSDPGRLITDPRSGRTYLKGRLLGKGGFARCYEATDTETGSAYAVKVIPQSRVAKPHQREKILNEIELHRDLQHRHIVRFSHHFEDADNIYIFLELCSRKSLAHIWKARHTLLEPEVRYYLRQILSGLKYLHQRGILHRDLKLGNFFITENMELKVGDFGLAARLEPPEQRKKTICGTPNYVAPEVLLRQGHGPEADVWSLGCVMYTLLCGSPPFETADLKETYRCIKQVHYTLPASLSLPARQLLAAILRASPRDRPSIDQILRHDFFTKGYTPDRLPISSCVTVPDLTPPNPARSLFAKVTKSLFGRKKKSKNHAQERDEVSGLVSGLMRTSVGHQDARPEAPAASGPAPVSLVETAPEDSSPRGTLASSGDGFEEGLTVATVVESALCALRNCIAFMPPAEQNPAPLAQPEPLVWVSKWVDYSNKFGFGYQLSSRRVAVLFNDGTHMALSANRKTVHYNPTSTKHFSFSVGAVPRALQPQLGILRYFASYMEQHLMKGGDLPSVEEVEVPAPPLLLQWVKTDQALLMLFSDGTVQVNFYGDHTKLILSGWEPLLVTFVARNRSACTYLASHLRQLGCSPDLRQRLRYALRLLRDRSPA
  
Inhibitor
Name:
BDBM50362981
Synonyms:
CHEMBL1945171
Type:
Small organic molecule
Emp. Form.:
C24H26ClN5S
Mol. Mass.:
452.015
SMILES:
CN(C)CCCc1ccc(C)c(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)c1
Structure:
Search PDB for entries with ligand similarity: