| Reaction Details |
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 | Report a problem with these data |
| Target | Ribosomal protein S6 kinase alpha-3 |
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| Ligand | BDBM286084 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Radioisotope assay |
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| IC50 | 94000±n/a 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-α]pyrazine-2-carboxamides as RSK inhibitors US Patent US10081632 Publication Date 9/25/2018 |
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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 |
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| 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 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 83740.03 |
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| Organism: | Homo sapiens (Human) |
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| 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. |
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| Residue: | 740 |
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| Sequence: | MPLAQLADPWQKMAVESPSDSAENGQQIMDEPMGEEEINPQTEEVSIKEIAITHHVKEGH
EKADPSQFELLKVLGQGSFGKVFLVKKISGSDARQLYAMKVLKKATLKVRDRVRTKMERD
ILVEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALA
LDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKESIDHEKKAYSFCGTVEYMAPEVV
NRRGHTQSADWWSFGVLMFEMLTGTLPFQGKDRKETMTMILKAKLGMPQFLSPEAQSLLR
MLFKRNPANRLGAGPDGVEEIKRHSFFSTIDWNKLYRREIHPPFKPATGRPEDTFYFDPE
FTAKTPKDSPGIPPSANAHQLFRGFSFVAITSDDESQAMQTVGVHSIVQQLHRNSIQFTD
GYEVKEDIGVGSYSVCKRCIHKATNMEFAVKIIDKSKRDPTEEIEILLRYGQHPNIITLK
DVYDDGKYVYVVTELMKGGELLDKILRQKFFSEREASAVLFTITKTVEYLHAQGVVHRDL
KPSNILYVDESGNPESIRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDAACD
IWSLGVLLYTMLTGYTPFANGPDDTPEEILARIGSGKFSLSGGYWNSVSDTAKDLVSKML
HVDPHQRLTAALVLRHPWIVHWDQLPQYQLNRQDAPHLVKGAMAATYSALNRNQSPVLEP
VGRSTLAQRRGIKKITSTAL
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| BDBM286084 |
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| n/a |
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| Name | BDBM286084 |
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| Synonyms: | (R)-1-benzyl-N-(4-methyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indol-7-yl)-1H-pyrazole-4-carboxamide | BDBM286088 | US10081632, Compound 11 | US10758530, Compound 11 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H21N5O2 |
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| Mol. Mass. | 399.4451 |
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| SMILES | C[C@@H]1CNC(=O)c2cc3ccc(NC(=O)c4cnn(Cc5ccccc5)c4)cc3n12 |r| |
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| Structure | 
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