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Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM50362979
Substrate
n/a
Meas. Tech.
ChEMBL_800413 (CHEMBL1948344)
IC50
140±n/a nM
Citation
 Duffey, MO; Vos, TJ; Adams, R; Alley, J; Anthony, J; Barrett, C; Bharathan, I; Bowman, D; Bump, NJ; Chau, R; Cullis, C; Driscoll, DL; Elder, A; Forsyth, N; Frazer, J; Guo, J; Guo, L; Hyer, ML; Janowick, D; Kulkarni, B; Lai, SJ; Lasky, K; Li, G; Li, J; Liao, D; Little, J; Peng, B; Qian, MG; Reynolds, DJ; Rezaei, M; Scott, MP; Sells, TB; Shinde, V; Shi, QJ; Sintchak, MD; Soucy, F; Sprott, KT; Stroud, SG; Nestor, M; Visiers, I; Weatherhead, G; Ye, Y; D'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:
BDBM50362979
Synonyms:
CHEMBL1945173
Type:
Small organic molecule
Emp. Form.:
C24H26ClN5OS
Mol. Mass.:
468.014
SMILES:
COc1ccc(CCCN(C)C)cc1Nc1ncc2CC(=S)Nc3cc(Cl)ccc3-c2n1
Structure:
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