Reaction Details |
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Target | Aurora kinase A |
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Ligand | BDBM50347659 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_756092 (CHEMBL1804348) |
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IC50 | 290±n/a nM |
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Citation | Katz, JD; Jewell, JP; Guerin, DJ; Lim, J; Dinsmore, CJ; Deshmukh, SV; Pan, BS; Marshall, CG; Lu, W; Altman, MD; Dahlberg, WK; Davis, L; Falcone, D; Gabarda, AE; Hang, G; Hatch, H; Holmes, R; Kunii, K; Lumb, KJ; Lutterbach, B; Mathvink, R; Nazef, N; Patel, SB; Qu, X; Reilly, JF; Rickert, KW; Rosenstein, C; Soisson, SM; Spencer, KB; Szewczak, AA; Walker, D; Wang, W; Young, J; Zeng, Q Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer. J Med Chem54:4092-108 (2011) [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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BDBM50347659 |
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n/a |
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Name | BDBM50347659 |
Synonyms: | CHEMBL1802916 | MK-2461 |
Type | Small organic molecule |
Emp. Form. | C24H25N5O5S |
Mol. Mass. | 495.551 |
SMILES | CN(C[C@@H]1COCCO1)S(=O)(=O)Nc1ccc2ccc3ncc(cc3c(=O)c2c1)-c1cnn(C)c1 |r| |
Structure |
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