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TargetRibosomal protein S6 kinase alpha-3
LigandBDBM50361851
Substrate/Competitorn/a
Meas. Tech.ChEMBL_799761
IC50 4±n/a nM
Citation Boyer, SJBurke, JGuo, XKirrane, TMSnow, RJZhang, YSarko, CSoleymanzadeh, LSwinamer, AWestbrook, JDicapua, FPadyana, ACogan, DGao, AXiong, ZMadwed, JBKashem, MKugler, SO'Neill, MM Indole RSK inhibitors. Part 1: discovery and initial SAR. Bioorg Med Chem Lett22:733-7 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Ribosomal protein S6 kinase alpha-3
Name:Ribosomal protein S6 kinase alpha-1/alpha-3
Synonyms:90 kDa ribosomal protein S6 kinase 3 | ISPK-1 | MAP kinase-activated protein kinase 1b | MAPKAPK1B | RPS6KA3(Kin.Dom.1 - N-terminal) | Ribosomal S6 kinase 2 (RSK2) | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha-3 (RSK2) | S6K-alpha 3 | insulin-stimulated protein kinase 1 | p90 ribosomal s6 kinase (RSK2) | p90-RSK 3 | 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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BDBM50361851
NameBDBM50361851
Synonyms:CHEMBL1938803 | US9150577, 55
TypeSmall organic molecule
Emp. Form.C20H17N5O2
Mol. Mass.359.3813
SMILESO=C(Nc1nc2ccccc2[nH]1)c1ccc2cc3C(=O)NCCCn3c2c1
Structure
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n/a