Reaction Details |
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Target | Ribosomal protein S6 kinase alpha-4 |
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Ligand | BDBM50401152 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_881458 (CHEMBL2214445) |
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IC50 | <10000±n/a nM |
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Citation | Sunose, M; Bell, K; Ellard, K; Bergamini, G; Neubauer, G; Werner, T; Ramsden, N Discovery of 5-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-(tert-butyl)pyridine-3-sulfonamide (CZC24758), as a potent, orally bioavailable and selective inhibitor of PI3K for the treatment of inflammatory disease. Bioorg Med Chem Lett22:4613-8 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Ribosomal protein S6 kinase alpha-4 |
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Name: | Ribosomal protein S6 kinase alpha-4 |
Synonyms: | 90 kDa ribosomal protein S6 kinase 4 | KS6A4_HUMAN | MSK2 | Mitogen- and Stress-Activated Protein Kinase 2 (MSK2) | Nuclear mitogen- and stress-activated protein kinase 2 | RPS6KA4 | RPS6KA4(Kin.Dom.1 - N-terminal) | RSKB | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha 4 | Ribosomal protein S6 kinase alpha-4 | Ribosomal protein kinase B |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 85620.38 |
Organism: | Homo sapiens (Human) |
Description: | Recombinant MSK2 was phosphorylated by incubation with active p38alpha before assays. |
Residue: | 772 |
Sequence: | MGDEDDDESCAVELRITEANLTGHEEKVSVENFELLKVLGTGAYGKVFLVRKAGGHDAGK
LYAMKVLRKAALVQRAKTQEHTRTERSVLELVRQAPFLVTLHYAFQTDAKLHLILDYVSG
GEMFTHLYQRQYFKEAEVRVYGGEIVLALEHLHKLGIIYRDLKLENVLLDSEGHIVLTDF
GLSKEFLTEEKERTFSFCGTIEYMAPEIIRSKTGHGKAVDWWSLGILLFELLTGASPFTL
EGERNTQAEVSRRILKCSPPFPPRIGPVAQDLLQRLLCKDPKKRLGAGPQGAQEVRNHPF
FQGLDWVALAARKIPAPFRPQIRSELDVGNFAEEFTRLEPVYSPPGSPPPGDPRIFQGYS
FVAPSILFDHNNAVMTDGLEAPGAGDRPGRAAVARSAMMQDSPFFQQYELDLREPALGQG
SFSVCRRCRQRQSGQEFAVKILSRRLEANTQREVAALRLCQSHPNVVNLHEVHHDQLHTY
LVLELLRGGELLEHIRKKRHFSESEASQILRSLVSAVSFMHEEAGVVHRDLKPENILYAD
DTPGAPVKIIDFGFARLRPQSPGVPMQTPCFTLQYAAPELLAQQGYDESCDLWSLGVILY
MMLSGQVPFQGASGQGGQSQAAEIMCKIREGRFSLDGEAWQGVSEEAKELVRGLLTVDPA
KRLKLEGLRGSSWLQDGSARSSPPLRTPDVLESSGPAVRSGLNATFMAFNRGKREGFFLK
SVENAPLAKRRKQKLRSATASRRGSPAPANPGRAPVASKGAPRRANGPLPPS
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BDBM50401152 |
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n/a |
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Name | BDBM50401152 |
Synonyms: | CHEMBL2205766 |
Type | Small organic molecule |
Emp. Form. | C15H18N6O2S |
Mol. Mass. | 346.407 |
SMILES | CC(C)(C)NS(=O)(=O)c1cncc(c1)-c1ccn2nc(N)nc2c1 |
Structure |
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