Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM50362986
Substrate
n/a
Meas. Tech.
ChEMBL_800413 (CHEMBL1948344)
IC50
7±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:
BDBM50362986
Synonyms:
CHEMBL1945501
Type:
Small organic molecule
Emp. Form.:
C23H23ClFN5S
Mol. Mass.:
455.979
SMILES:
CN(C)CCCc1cc(Nc2ncc3CC(=S)Nc4cc(Cl)ccc4-c3n2)ccc1F
Structure:
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