Reaction Details |
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Target | Serine/threonine-protein kinase PLK3 |
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Ligand | BDBM50318064 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_631391 (CHEMBL1109143) |
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IC50 | 49±n/a nM |
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Citation | Beria, I; Ballinari, D; Bertrand, JA; Borghi, D; Bossi, RT; Brasca, MG; Cappella, P; Caruso, M; Ceccarelli, W; Ciavolella, A; Cristiani, C; Croci, V; De Ponti, A; Fachin, G; Ferguson, RD; Lansen, J; Moll, JK; Pesenti, E; Posteri, H; Perego, R; Rocchetti, M; Storici, P; Volpi, D; Valsasina, 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 Chem53:3532-51 (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 |
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
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BDBM50318064 |
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n/a |
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Name | BDBM50318064 |
Synonyms: | 8-{[2-(Acetylamino)phenyl]amino}-1-methyl-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1097373 |
Type | Small organic molecule |
Emp. Form. | C19H19N7O2 |
Mol. Mass. | 377.3999 |
SMILES | CC(=O)Nc1ccccc1Nc1ncc2CCc3c(nn(C)c3-c2n1)C(N)=O |
Structure |
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