Reaction Details |
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Target | Serine/threonine-protein kinase PLK1 |
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Ligand | BDBM50329917 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_675877 (CHEMBL1272694) |
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IC50 | 127±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 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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BDBM50329917 |
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n/a |
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Name | BDBM50329917 |
Synonyms: | 4-(3-(3-carbamoyl-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazolin-8-ylamino)-4-(trifluoromethoxy)phenyl)-1-methylpiperazine 1-oxide | CHEMBL1271645 |
Type | Small organic molecule |
Emp. Form. | C23H25F3N8O3 |
Mol. Mass. | 518.4916 |
SMILES | Cn1nc(C(N)=O)c2CCc3cnc(Nc4cc(ccc4OC(F)(F)F)N4CC[N+](C)([O-])CC4)nc3-c12 |
Structure |
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