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Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM28219
Substrate
PLK Substrate Peptide
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
7.2±n/a
Temperature
295.15±n/a K
IC50
250±n/a nM
Citation
Emmitte, KA; Adjebang, GM; Andrews, CW; Alberti, JG; Bambal, R; Chamberlain, SD; Davis-Ward, RG; Dickson, HD; Hassler, DF; Hornberger, KR; Jackson, JR; Kuntz, KW; Lansing, TJ; Mook, RA; Nailor, KE; Pobanz, MA; Smith, SC; Sung, CM; Cheung, M Design of potent thiophene inhibitors of polo-like kinase 1 with improved solubility and reduced protein binding. Bioorg Med Chem Lett 19:1694-7 (2009) [PubMed] Article
More Info.:
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:
BDBM28219
Synonyms:
3-[(1R)-1-(2-chlorophenyl)ethoxy]-5-(6-{[(4R)-1-methylazepan-4-yl]oxy}-1H-1,3-benzodiazol-1-yl)thiophene-2-carboxamide | benzimidazole thiophene carboxamide, 27
Type:
Small organic molecule
Emp. Form.:
C27H29ClN4O3S
Mol. Mass.:
525.062
SMILES:
C[C@@H](Oc1cc(sc1C(N)=O)-n1cnc2ccc(O[C@@H]3CCCN(C)CC3)cc12)c1ccccc1Cl |r|
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