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Target
Aurora kinase A
Ligand
BDBM50181537
Substrate
n/a
Meas. Tech.
ChEMBL_420088 (CHEMBL873731)
IC50
2±n/a nM
Citation
Jung, FH; Pasquet, G; Lambert-van der Brempt, C; Lohmann, JJ; Warin, N; Renaud, F; Germain, H; De Savi, C; Roberts, N; Johnson, T; Dousson, C; Hill, GB; Mortlock, AA; Heron, N; Wilkinson, RW; Wedge, SR; Heaton, SP; Odedra, R; Keen, NJ; Green, S; Brown, E; Thompson, K; Brightwell, S Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J Med Chem 49:955-70 (2006) [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:
BDBM50181537
Synonyms:
CHEMBL201197 | N-(2,3-difluorophenyl)-2-{2-[(7-{3-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]propoxy}-6-methoxyquinazolin-4-yl)amino]-1,3-thiazol-5-yl}acetamide
Type:
Small organic molecule
Emp. Form.:
C28H30F2N6O4S
Mol. Mass.:
584.637
SMILES:
COc1cc2c(Nc3ncc(CC(=O)Nc4cccc(F)c4F)s3)ncnc2cc1OCCCN1CCC[C@H]1CO