Reaction Details |
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Target | Ribosomal protein S6 kinase alpha-3 |
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Ligand | BDBM286078 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Radioisotope assay |
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IC50 | >10000±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 |
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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BDBM286078 |
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n/a |
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Name | BDBM286078 |
Synonyms: | 1-Benzyl-N-(3-(morpholinomethyl)benzo[b]thiophen-5-yl)-1H-pyrazole-4-carboxamide | US10081632, Compound 5 | US10758530, Compound 5 | US9771366, Compound 5 |
Type | Small organic molecule |
Emp. Form. | C24H24N4O2S |
Mol. Mass. | 432.538 |
SMILES | O=C(Nc1ccc2scc(CN3CCOCC3)c2c1)c1cnn(Cc2ccccc2)c1 |
Structure |
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