Reaction Details |
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Target | Serine/threonine-protein kinase PLK1 |
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Ligand | BDBM50343565 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_747145 (CHEMBL1777511) |
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IC50 | 83±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 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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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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