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TargetRibosomal protein S6 kinase alpha-3
LigandBDBM342166
Substrate/Competitorn/a
Meas. Tech.Kinase Assay
IC50 6.0±0.0 nM
Citation Dunn, SEJayanthan, ANagireddy, JRAnnedi, SVan Drie, JHDaynard, TSHuynh, M Substituted tetrahydropyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors US Patent US9771366 Publication Date 9/26/2017
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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  Blast E-value cutoff:
BDBM342166
NameBDBM342166
Synonyms:(R)-1-benzyl-N-(9-methyl-6-oxo-6,7,8,9-tetrahydropyrido[3',2':4,5]pyrrolo[1,2-a]pyrazin-2-yl)-1H-pyrazole-4-carboxamide | US9771366, Compound 15
TypeSmall organic molecule
Emp. Form.C23H21N5O2
Mol. Mass.399.4451
SMILESC[C@@H]1CNC(=O)c2cc3cc(NC(=O)c4cnn(Cc5ccccc5)c4)ccc3n12 |r|
Structure
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