Reaction Details Report a problem with these data
Target
Aurora kinase A
Ligand
BDBM31555
Substrate
CHOCKtide
Meas. Tech.
Kinase SPA Assay
Temperature
298.15±n/a K
IC50
855±n/a nM
Comments
extracted
Citation
Brasca, MG; Amboldi, N; Ballinari, D; Cameron, A; Casale, E; Cervi, G; Colombo, M; Colotta, F; Croci, V; D'Alessio, R; Fiorentini, F; Isacchi, A; Mercurio, C; Moretti, W; Panzeri, A; Pastori, W; Pevarello, P; Quartieri, F; Roletto, F; Traquandi, G; Vianello, P; Vulpetti, A; Ciomei, M Identification of N,1,4,4-Tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide (PHA-848125), a Potent, Orally Available Cyclin Dependent Kinase Inhibitor. J Med Chem 52:5152-63 (2009) [PubMed] Article
More Info.:
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:
BDBM31555
Synonyms:
pyrazolo[4,3-h]quinazoline-3-carboxamide, 38
Type:
Small organic molecule
Emp. Form.:
C22H27N7O
Mol. Mass.:
405.4961
SMILES:
CNC(=O)c1nn(C)c-2c1C(C)(C)Cc1cnc(Nc3ccc(cc3)N(C)C)nc-21
Substrate
Name:
CHOCKtide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
889.06
Organism:
n/a
Description:
n/a
Residue:
7
Sequence:
LRRWSLG