Reaction Details |
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Target | Serine/threonine-protein kinase PLK1 |
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Ligand | BDBM50318095 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_631389 (CHEMBL1109141) |
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IC50 | 51±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 PLK1 |
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Name: | Serine/threonine-protein kinase PLK1 |
Synonyms: | PLK | PLK-1 | PLK1 | PLK1_HUMAN | Polo-like kinase 1 (PlK1) | Polo-like kinase 1 (Plk-1) | STPK13 | Serine/threonine-protein kinase (PLK1) | Serine/threonine-protein kinase 13 | polo-like kinase |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 68277.16 |
Organism: | Homo sapiens (Human) |
Description: | P53350 |
Residue: | 603 |
Sequence: | MSAAVTAGKLARAPADPGKAGVPGVAAPGAPAAAPPAKEIPEVLVDPRSRRRYVRGRFLG
KGGFAKCFEISDADTKEVFAGKIVPKSLLLKPHQREKMSMEISIHRSLAHQHVVGFHGFF
EDNDFVFVVLELCRRRSLLELHKRRKALTEPEARYYLRQIVLGCQYLHRNRVIHRDLKLG
NLFLNEDLEVKIGDFGLATKVEYDGERKKTLCGTPNYIAPEVLSKKGHSFEVDVWSIGCI
MYTLLVGKPPFETSCLKETYLRIKKNEYSIPKHINPVAASLIQKMLQTDPTARPTINELL
NDEFFTSGYIPARLPITCLTIPPRFSIAPSSLDPSNRKPLTVLNKGLENPLPERPREKEE
PVVRETGEVVDCHLSDMLQQLHSVNASKPSERGLVRQEEAEDPACIPIFWVSKWVDYSDK
YGLGYQLCDNSVGVLFNDSTRLILYNDGDSLQYIERDGTESYLTVSSHPNSLMKKITLLK
YFRNYMSEHLLKAGANITPREGDELARLPYLRTWFRTRSAIILHLSNGSVQINFFQDHTK
LILCPLMAAVTYIDEKRDFRTYRLSLLEEYGCCKELASRLRYARTMVDKLLSSRSASNRL
KAS
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BDBM50318095 |
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n/a |
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Name | BDBM50318095 |
Synonyms: | 1-Methyl-8-{[3-(trifluoromethyl)phenyl]amino}-4,5-dihydro-1Hpyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1097424 |
Type | Small organic molecule |
Emp. Form. | C18H15F3N6O |
Mol. Mass. | 388.3465 |
SMILES | Cn1nc(C(N)=O)c2CCc3cnc(Nc4cccc(c4)C(F)(F)F)nc3-c12 |
Structure |
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