Reaction Details |
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Target | Aurora kinase A |
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Ligand | BDBM50183019 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1586341 (CHEMBL3820511) |
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IC50 | >50000±n/a nM |
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Citation | Laufer, R; Li, SW; Liu, Y; Ng, G; Lang, Y; Feher, M; Brokx, R; Beletskaya, I; Hodgson, R; Mao, G; Plotnikova, O; Awrey, DE; Mason, JM; Wei, X; Lin, DC; Che, Y; Kiarash, R; Madeira, B; Fletcher, GC; Mak, TW; Bray, MR; Pauls, HW Discovery of 4-(4-aminopyrazolo[1,5-a][1,3,5]triazin-8-yl)benzamides as novel, highly potent and selective, orally bioavailable inhibitors of Tyrosine Threonine Kinase, TTK. Bioorg Med Chem Lett26:3562-6 (2016) [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 | 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: | MDRSKENCISGPVKATAPVGGPKRVLVTQQFPCQNPLPVNSGQAQRVLCPSNSSQRIPLQ
AQKLVSSHKPVQNQKQKQLQATSVPHPVSRPLNNTQKSKQPLPSAPENNPEEELASKQKN
EESKKRQWALEDFEIGRPLGKGKFGNVYLAREKQSKFILALKVLFKAQLEKAGVEHQLRR
EVEIQSHLRHPNILRLYGYFHDATRVYLILEYAPLGTVYRELQKLSKFDEQRTATYITEL
ANALSYCHSKRVIHRDIKPENLLLGSAGELKIADFGWSVHAPSSRRTTLCGTLDYLPPEM
IEGRMHDEKVDLWSLGVLCYEFLVGKPPFEANTYQETYKRISRVEFTFPDFVTEGARDLI
SRLLKHNPSQRPMLREVLEHPWITANSSKPSNCQNKESASKQS
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BDBM50183019 |
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n/a |
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Name | BDBM50183019 |
Synonyms: | CHEMBL3819210 |
Type | Small organic molecule |
Emp. Form. | C28H30N6O3 |
Mol. Mass. | 498.5762 |
SMILES | Cc1cc(ccc1C(=O)NC1CC1)-c1cnn2c(NCC3CCOCC3)nc(Oc3ccccc3)nc12 |
Structure |
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