Reaction Details |
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Target | Ribosomal protein S6 kinase alpha-3 |
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Ligand | BDBM50361837 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_799760 (CHEMBL1941466) |
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IC50 | 1630±n/a nM |
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Citation | Boyer, SJ; Burke, J; Guo, X; Kirrane, TM; Snow, RJ; Zhang, Y; Sarko, C; Soleymanzadeh, L; Swinamer, A; Westbrook, J; Dicapua, F; Padyana, A; Cogan, D; Gao, A; Xiong, Z; Madwed, JB; Kashem, M; Kugler, S; O'Neill, MM Indole RSK inhibitors. Part 1: discovery and initial SAR. Bioorg Med Chem Lett22:733-7 (2011) [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-3 |
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Name: | Ribosomal protein S6 kinase alpha-3 |
Synonyms: | 90 kDa ribosomal protein S6 kinase 3 | ISPK-1 | ISPK1 | KS6A3_HUMAN | MAP kinase-activated protein kinase 1b | MAPKAPK1B | RPS6KA3 | RPS6KA3(Kin.Dom.1 - N-terminal) | RSK2 | Ribosomal S6 kinase 2 (RSK2) | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha-1/alpha-3 | Ribosomal protein S6 kinase alpha-3 (RSK2) | Ribosomal protein S6 kinase alpha-3 (RSK3) | S6K-alpha 3 | insulin-stimulated protein kinase 1 | p90 ribosomal s6 kinase (RSK2) | p90-RSK 3 | p90RSK | pp90RSK2 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 83740.03 |
Organism: | Homo sapiens (Human) |
Description: | The human RSK2 sequence differed from the Genbank entry NM_004586 at one residue, V45G. The protein was cloned and purified from baculovirus expression system. |
Residue: | 740 |
Sequence: | MPLAQLADPWQKMAVESPSDSAENGQQIMDEPMGEEEINPQTEEVSIKEIAITHHVKEGH
EKADPSQFELLKVLGQGSFGKVFLVKKISGSDARQLYAMKVLKKATLKVRDRVRTKMERD
ILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALA
LDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKESIDHEKKAYSFCGTVEYMAPEVV
NRRGHTQSADWWSFGVLMFEMLTGTLPFQGKDRKETMTMILKAKLGMPQFLSPEAQSLLR
MLFKRNPANRLGAGPDGVEEIKRHSFFSTIDWNKLYRREIHPPFKPATGRPEDTFYFDPE
FTAKTPKDSPGIPPSANAHQLFRGFSFVAITSDDESQAMQTVGVHSIVQQLHRNSIQFTD
GYEVKEDIGVGSYSVCKRCIHKATNMEFAVKIIDKSKRDPTEEIEILLRYGQHPNIITLK
DVYDDGKYVYVVTELMKGGELLDKILRQKFFSEREASAVLFTITKTVEYLHAQGVVHRDL
KPSNILYVDESGNPESIRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDAACD
IWSLGVLLYTMLTGYTPFANGPDDTPEEILARIGSGKFSLSGGYWNSVSDTAKDLVSKML
HVDPHQRLTAALVLRHPWIVHWDQLPQYQLNRQDAPHLVKGAMAATYSALNRNQSPVLEP
VGRSTLAQRRGIKKITSTAL
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BDBM50361837 |
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n/a |
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Name | BDBM50361837 |
Synonyms: | CHEMBL1938774 |
Type | Small organic molecule |
Emp. Form. | C18H16N4O2 |
Mol. Mass. | 320.3452 |
SMILES | CC1CNC(=O)c2cc3ccc(cc3n12)C(=O)Nc1cccnc1 |
Structure |
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