Reaction Details |
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Target | Aurora kinase B |
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Ligand | BDBM24721 |
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Substrate/Competitor | Histone H3 |
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Meas. Tech. | Enzyme Inhibition Assay |
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pH | 7.5±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 5±n/a nM |
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Citation | Rawson, TE; Rüth, M; Blackwood, E; Burdick, D; Corson, L; Dotson, J; Drummond, J; Fields, C; Georges, GJ; Goller, B; Halladay, J; Hunsaker, T; Kleinheinz, T; Krell, HW; Li, J; Liang, J; Limberg, A; McNutt, A; Moffat, J; Phillips, G; Ran, Y; Safina, B; Ultsch, M; Walker, L; Wiesmann, C; Zhang, B; Zhou, A; Zhu, BY; Rüger, P; Cochran, AG A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability. J Med Chem51:4465-75 (2008) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Aurora kinase B |
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Name: | Aurora kinase B |
Synonyms: | AIK2 | AIM-1 | AIM1 | AIRK2 | ARK2 | AURKB | AURKB_HUMAN | Aurora B kinase (aurB) | Aurora B-INCENP | Aurora kinase 2 | Aurora kinase B (AURKB) | Aurora-related kinase 2 | STK-1 | STK1 | STK12 | STK5 | Serine/threonine-protein kinase aurora B |
Type: | Protein |
Mol. Mass.: | 39327.72 |
Organism: | Homo sapiens (Human) |
Description: | Q96GD4 |
Residue: | 344 |
Sequence: | MAQKENSYPWPYGRQTAPSGLSTLPQRVLRKEPVTPSALVLMSRSNVQPTAAPGQKVMEN
SSGTPDILTRHFTIDDFEIGRPLGKGKFGNVYLAREKKSHFIVALKVLFKSQIEKEGVEH
QLRREIEIQAHLHHPNILRLYNYFYDRRRIYLILEYAPRGELYKELQKSCTFDEQRTATI
MEELADALMYCHGKKVIHRDIKPENLLLGLKGELKIADFGWSVHAPSLRRKTMCGTLDYL
PPEMIEGRMHNEKVDLWCIGVLCYELLVGNPPFESASHNETYRRIVKVDLKFPASVPMGA
QDLISKLLRHNPSERLPLAQVSAHPWVRANSRRVLPPSALQSVA
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BDBM24721 |
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Histone H3 |
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Name: | Histone H3 (aa 1-18) |
Synonyms: | GST fusion of N-terminus of Histone H3 (aa 1-18) | H31_HUMAN | H3C1 | H3FA | H3FB | H3FC HIST1H3C | H3FD | H3FF | H3FH | H3FI | H3FJ | H3FK | H3FL | HIST1H3A | HIST1H3B | HIST1H3D | HIST1H3E | HIST1H3F | HIST1H3G | HIST1H3H | HIST1H3I | HIST1H3J | Histone H3 |
Type: | Peptide |
Mol. Mass.: | 1951.30 |
Organism: | Homo sapiens (Human) |
Description: | P68431 (aa 1-18) |
Residue: | 18 |
Sequence: | |