Target
Serine/threonine-protein kinase PLK3
Ligand
BDBM50318081
Substrate
n/a
Meas. Tech.
ChEMBL_631391 (CHEMBL1109143)
IC50
13±n/a nM
Citation
 Beria, IBallinari, DBertrand, JABorghi, DBossi, RTBrasca, MGCappella, PCaruso, MCeccarelli, WCiavolella, ACristiani, CCroci, VDe Ponti, AFachin, GFerguson, RDLansen, JMoll, JKPesenti, EPosteri, HPerego, RRocchetti, MStorici, PVolpi, DValsasina, B Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J Med Chem 53:3532-51 (2010) [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:
BDBM50318081
Synonyms:
8-[(2-Methoxyphenyl)amino]-1-methyl-4,5-dihydro-1H-pyrazolo-[4,3-h]quinazoline-3-carboxamide | CHEMBL1094135
Type:
Small organic molecule
Emp. Form.:
C18H18N6O2
Mol. Mass.:
350.3745
SMILES:
COc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O
Structure:
Search PDB for entries with ligand similarity: