| Reaction Details |
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 | Report a problem with these data |
| Target | Serine/threonine-protein kinase PLK3 |
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| Ligand | BDBM50329929 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_675879 (CHEMBL1272696) |
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| IC50 | 182±n/a nM |
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| Citation |  Beria, I; Valsasina, B; Brasca, MG; Ceccarelli, W; Colombo, M; Cribioli, S; Fachin, G; Ferguson, RD; Fiorentini, F; Gianellini, LM; Giorgini, ML; Moll, JK; Posteri, H; Pezzetta, D; Roletto, F; Sola, F; Tesei, D; Caruso, M 4,5-Dihydro-1H-pyrazolo[4,3-h]quinazolines as potent and selective Polo-like kinase 1 (PLK1) inhibitors. Bioorg Med Chem Lett20:6489-94 (2010) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Serine/threonine-protein kinase PLK3 |
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| Name: | Serine/threonine-protein kinase PLK3 |
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| 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 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 71655.17 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Enzyme assays were using PLK3 purified from baculovirus-infected Trichoplusia ni cells expressing full-length PLK3. |
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| Residue: | 646 |
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| Sequence: | MEPAAGFLSPRPFQRAAAAPAPPAGPGPPPSALRGPELEMLAGLPTSDPGRLITDPRSGR
TYLKGRLLGKGGFARCYEATDTETGSAYAVKVIPQSRVAKPHQREKILNEIELHRDLQHR
HIVRFSHHFEDADNIYIFLELCSRKSLAHIWKARHTLLEPEVRYYLRQILSGLKYLHQRG
ILHRDLKLGNFFITENMELKVGDFGLAARLEPPEQRKKTICGTPNYVAPEVLLRQGHGPE
ADVWSLGCVMYTLLCGSPPFETADLKETYRCIKQVHYTLPASLSLPARQLLAAILRASPR
DRPSIDQILRHDFFTKGYTPDRLPISSCVTVPDLTPPNPARSLFAKVTKSLFGRKKKSKN
HAQERDEVSGLVSGLMRTSVGHQDARPEAPAASGPAPVSLVETAPEDSSPRGTLASSGDG
FEEGLTVATVVESALCALRNCIAFMPPAEQNPAPLAQPEPLVWVSKWVDYSNKFGFGYQL
SSRRVAVLFNDGTHMALSANRKTVHYNPTSTKHFSFSVGAVPRALQPQLGILRYFASYME
QHLMKGGDLPSVEEVEVPAPPLLLQWVKTDQALLMLFSDGTVQVNFYGDHTKLILSGWEP
LLVTFVARNRSACTYLASHLRQLGCSPDLRQRLRYALRLLRDRSPA
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| BDBM50329929 |
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| n/a |
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| Name | BDBM50329929 |
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| Synonyms: | 8-(5-(piperazin-1-yl)-2-(trifluoromethoxy)phenylamino)-1-vinyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1271870 |
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| Type | Small organic molecule |
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| Emp. Form. | C24H25F3N8O2 |
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| Mol. Mass. | 514.5029 |
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| SMILES | CN1CCN(CC1)c1ccc(OC(F)(F)F)c(Nc2ncc3CCc4c(nn(C=C)c4-c3n2)C(N)=O)c1 |
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| Structure | 
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