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Target
Aurora kinase A
Ligand
BDBM12986
Substrate
CHOCKtide
Meas. Tech.
Kinase SPA Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
452±n/a nM
Citation
 Fancelli, D; Moll, J; Varasi, M; Bravo, R; Artico, R; Berta, D; Bindi, S; Cameron, A; Candiani, I; Cappella, P; Carpinelli, P; Croci, W; Forte, B; Giorgini, ML; Klapwijk, J; Marsiglio, A; Pesenti, E; Rocchetti, M; Roletto, F; Severino, D; Soncini, C; Storici, P; Tonani, R; Zugnoni, P; Vianello, P 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem 49:7247-51 (2006) [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:
BDBM12986
Synonyms:
4-(4-methylpiperazin-1-yl)-N-{5-[(2S)-2-phenylpropanoyl]-1H,4H,5H,6H-pyrrolo[3,4-c]pyrazol-3-yl}benzamide | 5-Amido-pyrrolopyrazole 9e | CHEMBL217748
Type:
Small organic molecule
Emp. Form.:
C26H30N6O2
Mol. Mass.:
458.5554
SMILES:
C[C@H](C(=O)N1Cc2n[nH]c(NC(=O)c3ccc(cc3)N3CCN(C)CC3)c2C1)c1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
CHOCKtide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
889.06
Organism:
n/a
Description:
n/a
Residue:
7
Sequence:
LRRWSLG