Reaction Details |
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Target | Aurora kinase A |
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Ligand | BDBM50318092 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_631394 (CHEMBL1109146) |
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IC50 | 42±n/a nM |
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Citation | Beria, I; Ballinari, D; Bertrand, JA; Borghi, D; Bossi, RT; Brasca, MG; Cappella, P; Caruso, M; Ceccarelli, W; Ciavolella, A; Cristiani, C; Croci, V; De Ponti, A; Fachin, G; Ferguson, RD; Lansen, J; Moll, JK; Pesenti, E; Posteri, H; Perego, R; Rocchetti, M; Storici, P; Volpi, D; Valsasina, B Identification of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1 inhibitors. J Med Chem53:3532-51 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Aurora kinase A |
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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: | MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRVPLQ
AQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKN
EESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRR
EVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITEL
ANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEM
IEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLI
SRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
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BDBM50318092 |
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n/a |
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Name | BDBM50318092 |
Synonyms: | 8-(Phenylamino)-1-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | CHEMBL1095709 |
Type | Small organic molecule |
Emp. Form. | C18H15F3N6O |
Mol. Mass. | 388.3465 |
SMILES | NC(=O)c1nn(CC(F)(F)F)c-2c1CCc1cnc(Nc3ccccc3)nc-21 |
Structure |
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