Reaction Details
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Aurora kinase A
Ligand
BDBM50059440
Substrate
n/a
Meas. Tech.
ChEMBL_1460905 (CHEMBL3396725)
IC50
6.0±n/a nM
Citation
Carry, JC; Clerc, F; Minoux, H; Schio, L; Mauger, J; Nair, A; Parmantier, E; Le Moigne, R; Delorme, C; Nicolas, JP; Krick, A; Abécassis, PY; Crocq-Stuerga, V; Pouzieux, S; Delarbre, L; Maignan, S; Bertrand, T; Bjergarde, K; Ma, N; Lachaud, S; Guizani, H; Lebel, R; Doerflinger, G; Monget, S; Perron, S; Gasse, F; Angouillant-Boniface, O; Filoche-Rommé, B; Murer, M; Gontier, S; Prévost, C; Monteiro, ML; Combeau, C SAR156497, an exquisitely selective inhibitor of aurora kinases. J Med Chem 58:362-75 (2015) [PubMed] Article More Info.:
Target
Name:
Aurora kinase A
Synonyms:
AIK | AIRK1 | ARK-1 | 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 | STK15 GN | STK6 | Serine/threonine kinase 15 | Serine/threonine-protein kinase 15 | Serine/threonine-protein kinase 6 | Serine/threonine-protein kinase aurora A | Serine/threonine-protein kinase aurora-A | Synonyms=AIK | aurora-2 | hARK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
45830.98
Organism:
Homo sapiens (Human)
Description:
O14965
Residue:
403
Sequence:
MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRIPLQAQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKNEESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRREVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITELANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEMIEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLISRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
Inhibitor
Name:
BDBM50059440
Synonyms:
CHEMBL3393490
Type:
Small organic molecule
Emp. Form.:
C29H29N5O6S
Mol. Mass.:
575.635
SMILES:
CCOC(=O)c1[nH]cc2C(c3ccc(Sc4nc5ccccc5[nH]4)o3)C3=C(CN(CC3=O)C(=O)OC(C)(C)C)Nc12 |t:28|
Structure:
