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Target
Aurora kinase A
Ligand
BDBM26279
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Aurora B Kinase Inhibition Assay
Temperature
298.15±n/a K
Ki
2600±n/a nM
Comments
extracted
Citation
 Mortlock, AA; Foote, KM; Heron, NM; Jung, FH; Pasquet, G; Lohmann, JJ; Warin, N; Renaud, F; De Savi, C; Roberts, NJ; Johnson, T; Dousson, CB; Hill, GB; Perkins, D; Hatter, G; Wilkinson, RW; Wedge, SR; Heaton, SP; Odedra, R; Keen, NJ; Crafter, C; Brown, E; Thompson, K; Brightwell, S; Khatri, L; Brady, MC; Kearney, S; McKillop, D; Rhead, S; Parry, T; Green, S Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J Med Chem 50:2213-24 (2007) [PubMed]  Article 
Target
Name:
Aurora kinase A
Synonyms:
AIK | AIRK1 | ARK-1 | ARK1 | AURA | AURKA | AURKA_HUMAN | AYK1 | Aurora 2 | Aurora kinase A (AURA) | Aurora kinase A (AURKA) | Aurora kinase A (Aurora A) | Aurora kinase A (Aurora-2) | Aurora-related kinase 1 | Aurora/IPL1-related kinase 1 | BTAK | Breast tumor-amplified kinase | Breast-tumor-amplified kinase | IAK1 | STK15 | STK15 GN | STK6 | Serine/threonine kinase 15 | Serine/threonine-protein kinase 15 | Serine/threonine-protein kinase 6 | Serine/threonine-protein kinase aurora A | Serine/threonine-protein kinase aurora-A | Synonyms=AIK | aurora-2 | hARK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
45830.98
Organism:
Homo sapiens (Human)
Description:
O14965
Residue:
403
Sequence:
MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRIPLQAQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKNEESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRREVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITELANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEMIEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLISRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
  
Inhibitor
Name:
BDBM26279
Synonyms:
N-(3-cyanophenyl)-2-{3-[(7-{3-[4-(hydroxymethyl)piperidin-1-yl]propoxy}-6-methoxyquinazolin-4-yl)amino]-1H-pyrazol-5-yl}acetamide | pyrazoloquinazoline deriv., 13
Type:
Small organic molecule
Emp. Form.:
C30H34N8O4
Mol. Mass.:
570.6422
SMILES:
COc1cc2c(Nc3cc(CC(=O)Nc4cccc(c4)C#N)n[nH]3)ncnc2cc1OCCCN1CCC(CO)CC1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2374.22
Organism:
n/a
Description:
n/a
Residue:
20
Sequence:
ITINYLAHTETRALRRWSLG