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Target
Aurora kinase B
Ligand
BDBM26300
Substrate
Biotinylated Peptide Substrate
Meas. Tech.
Aurora B Kinase Inhibition Assay
Temperature
298.15±n/a K
Ki
<1±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
More Info.:
Target
Name:
Aurora kinase B
Synonyms:
AIK2 | AIM-1 | AIM1 | AIRK2 | ARK2 | AURKB | AURKB_HUMAN | Aurora B kinase (aurB) | Aurora B-INCENP | Aurora kinase 2 | Aurora kinase B (AURKB) | Aurora-related kinase 2 | STK-1 | STK1 | STK12 | STK5 | Serine/threonine-protein kinase aurora B
Type:
Protein
Mol. Mass.:
39327.72
Organism:
Human
Description:
Q96GD4
Residue:
344
Sequence:
MAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMENSSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEHQLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATIMEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYLPPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPMGAQDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA
Inhibitor
Name:
BDBM26300
Synonyms:
2-{3-[(7-{3-[ethyl(2-hydroxyethyl)amino]propoxy}quinazolin-4-yl)amino]-1H-pyrazol-5-yl}-N-(3-fluorophenyl)acetamide | CHEMBL215152 | cid_16007391 | pyrazoloquinazoline deriv., 34
Type:
Small organic molecule
Emp. Form.:
C26H30FN7O3
Mol. Mass.:
507.5599
SMILES:
CCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)n[nH]3)ncnc2c1
Substrate
Name:
Biotinylated Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2374.22
Organism:
n/a
Description:
n/a
Residue:
20
Sequence:
ITINYLAHTETRALRRWSLG