Target
Aurora kinase A
Ligand
BDBM26289
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Aurora B Kinase Inhibition Assay
Temperature
298.15±n/a K
Ki
110±n/a nM
Comments
extracted
Citation
 Mortlock, AAFoote, KMHeron, NMJung, FHPasquet, GLohmann, JJWarin, NRenaud, FDe Savi, CRoberts, NJJohnson, TDousson, CBHill, GBPerkins, DHatter, GWilkinson, RWWedge, SRHeaton, SPOdedra, RKeen, NJCrafter, CBrown, EThompson, KBrightwell, SKhatri, LBrady, MCKearney, SMcKillop, DRhead, SParry, TGreen, 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 | 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 | STK6 | Serine/threonine kinase 15 | Serine/threonine-protein kinase 6 | Serine/threonine-protein kinase aurora A | aurora-2 | hARK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
45830.98
Organism:
Homo sapiens (Human)
Description:
O14965
Residue:
403
Sequence:
MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRVPLQAQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKNEESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRREVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITELANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEMIEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLISRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
  
Inhibitor
Name:
BDBM26289
Synonyms:
N-(3-fluorophenyl)-2-{3-[(7-{3-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy}-6-methoxyquinazolin-4-yl)amino]-1H-pyrazol-5-yl}acetamide | pyrazoloquinazoline deriv., 23
Type:
Small organic molecule
Emp. Form.:
C28H32FN7O4
Mol. Mass.:
549.5966
SMILES:
COc1cc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)n[nH]3)ncnc2cc1OCCCN1CCC[C@@H]1CO |r|
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