Reaction Details |
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Target | Serine/threonine-protein kinase PLK3 |
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Ligand | BDBM50343565 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_747147 (CHEMBL1777513) |
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IC50 | 239±n/a nM |
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Citation | Beria, I; Bossi, RT; Brasca, MG; Caruso, M; Ceccarelli, W; Fachin, G; Fasolini, M; Forte, B; Fiorentini, F; Pesenti, E; Pezzetta, D; Posteri, H; Scolaro, A; Re Depaolini, S; Valsasina, 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 |
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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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BDBM50343565 |
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n/a |
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Name | BDBM50343565 |
Synonyms: | 1-methyl-8-(5-(pyrrolidin-2-ylamino)-2-(trifluoromethoxy)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1774332 |
Type | Small organic molecule |
Emp. Form. | C22H23F3N8O2 |
Mol. Mass. | 488.4656 |
SMILES | Cn1nc(C(N)=O)c2CCc3cnc(Nc4cc(NC5CCCN5)ccc4OC(F)(F)F)nc3-c12 |
Structure |
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