Reaction Details |
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Target | Ribosomal protein S6 kinase alpha-3 |
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Ligand | BDBM342166 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Kinase Assay |
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IC50 | 6.0±0.0 nM |
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Citation | Dunn, SE; Jayanthan, A; Nagireddy, JR; Annedi, S; Van Drie, JH; Daynard, TS; Huynh, 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 |
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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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BDBM342166 |
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n/a |
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Name | BDBM342166 |
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 |
Type | Small organic molecule |
Emp. Form. | C23H21N5O2 |
Mol. Mass. | 399.4451 |
SMILES | C[C@@H]1CNC(=O)c2cc3cc(NC(=O)c4cnn(Cc5ccccc5)c4)ccc3n12 |r| |
Structure |
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