Target
Aurora kinase A
Ligand
BDBM13534
Substrate
Not Specified
Meas. Tech.
In Vitro Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
0.6±n/a nM
Citation
 Harrington, EABebbington, DMoore, JRasmussen, RKAjose-Adeogun, AONakayama, TGraham, JADemur, CHercend, TDiu-Hercend, ASu, MGolec, JMMiller, KM VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med 10:262-7 (2004) [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:
BDBM13534
Synonyms:
CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]thio]phenyl]cyclopropanecarboxamide | VX-680 | VX680 | cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2ylsulphanyl]-phenyl}-amide
Type:
Small organic molecule
Emp. Form.:
C23H28N8OS
Mol. Mass.:
464.586
SMILES:
CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Not Specified
Synonyms:
n/a
Type:
n/a
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA