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TargetSerine/threonine-protein kinase PLK3
LigandBDBM50343566
Substrate/Competitorn/a
Meas. Tech.ChEMBL_747147 (CHEMBL1777513)
IC50 713±n/a nM
Citation Beria, IBossi, RTBrasca, MGCaruso, MCeccarelli, WFachin, GFasolini, MForte, BFiorentini, FPesenti, EPezzetta, DPosteri, HScolaro, ARe Depaolini, SValsasina, B NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett21:2969-74 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Serine/threonine-protein kinase PLK3
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:
MEPAAGFLSPRPFQRAAAAPAPPAGPGPPPSALRGPELEMLAGLPTSDPGRLITDPRSGR
TYLKGRLLGKGGFARCYEATDTETGSAYAVKVIPQSRVAKPHQREKILNEIELHRDLQHR
HIVRFSHHFEDADNIYIFLELCSRKSLAHIWKARHTLLEPEVRYYLRQILSGLKYLHQRG
ILHRDLKLGNFFITENMELKVGDFGLAARLEPPEQRKKTICGTPNYVAPEVLLRQGHGPE
ADVWSLGCVMYTLLCGSPPFETADLKETYRCIKQVHYTLPASLSLPARQLLAAILRASPR
DRPSIDQILRHDFFTKGYTPDRLPISSCVTVPDLTPPNPARSLFAKVTKSLFGRKKKSKN
HAQERDEVSGLVSGLMRTSVGHQDARPEAPAASGPAPVSLVETAPEDSSPRGTLASSGDG
FEEGLTVATVVESALCALRNCIAFMPPAEQNPAPLAQPEPLVWVSKWVDYSNKFGFGYQL
SSRRVAVLFNDGTHMALSANRKTVHYNPTSTKHFSFSVGAVPRALQPQLGILRYFASYME
QHLMKGGDLPSVEEVEVPAPPLLLQWVKTDQALLMLFSDGTVQVNFYGDHTKLILSGWEP
LLVTFVARNRSACTYLASHLRQLGCSPDLRQRLRYALRLLRDRSPA
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50343566
n/a
NameBDBM50343566
Synonyms:1-methyl-8-(5-(3-(4-methylpiperazin-1-yl)propylamino)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774333
TypeSmall organic molecule
Emp. Form.C26H32F3N9O2
Mol. Mass.559.5866
SMILESCN1CCN(CCCNc2ccc(OC(F)(F)F)c(Nc3ncc4CCc5c(nn(C)c5-c4n3)C(N)=O)c2)CC1
Structure
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