Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM25120
Substrate
PLK Substrate Peptide
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
9±n/a nM
Citation
 Emmitte, KAAndrews, CWBadiang, JGDavis-Ward, RGDickson, HDDrewry, DHEmerson, HKEpperly, AHHassler, DFKnick, VBKuntz, KWLansing, TJLinn, JAMook, RANailor, KESalovich, JMSpehar, GMCheung, M Discovery of thiophene inhibitors of polo-like kinase. Bioorg Med Chem Lett 19:1018-21 (2009) [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:
BDBM25120
Synonyms:
5-(5,6-dimethoxy-1H-1,3-benzodiazol-1-yl)-3-{[2-(trifluoromethyl)phenyl]methoxy}thiophene-2-carboxamide | BMCL191018 Compound 2 | thiophene deriv., 20
Type:
Small organic molecule
Emp. Form.:
C22H18F3N3O4S
Mol. Mass.:
477.456
SMILES:
COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
PLK Substrate Peptide
Synonyms:
n/a
Type:
Biotinylated peptide
Mol. Mass.:
1720.29
Organism:
n/a
Description:
n/a
Residue:
15
Sequence:
ITINAHSFNDTLDFD