| Reaction Details |
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| Target | Ribosomal S6 Kinase 1 (RSK-1) |
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| Ligand | oxadiazole-containing compound, 10 |
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| Substrate/Competitor | RSK1 Substrate Peptide |
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| Meas. Tech. | In Vitro Kinase Inhibition Assay |
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| pH | 7.2±n/a |
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| Temperature | 303.15±n/a K |
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| IC50 | 44±n/a nM |
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| Citation |  Heerding, DA; Rhodes, N; Leber, JD; Clark, TJ; Keenan, RM; Lafrance, LV; Li, M; Safonov, IG; Takata, DT; Venslavsky, JW; Yamashita, DS; Choudhry, AE; Copeland, RA; Lai, Z; Schaber, MD; Tummino, PJ; Strum, SL; Wood, ER; Duckett, DR; Eberwein, D; Knick, VB; Lansing, TJ; McConnell, RT; Zhang, S; Minthorn, EA; Concha, NO; Warren, GL; Kumar, R Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.J Med Chem.51:5663-79(2008)[PubMed] |
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| More Info. |
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, Solution Info
, Assay Method
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| Ribosomal S6 Kinase 1 (RSK-1) |
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| Name | Ribosomal S6 Kinase 1 (RSK-1) |
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| Synonyms | 90 kDa ribosomal protein S6 kinase 1 | p90-RSK 1 | pp90RSK1 | p90S6K | MAP kinase-activated protein kinase 1a | MAPKAPK1A | EC=2.7.11.1 | Ribosomal protein S6 kinase alpha-1 | S6K-alpha 1 |
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| Type | Serine/threonine-protein kinase |
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| Mol. Mass. | 82723 |
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| Organism | Homo sapiens (human) |
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| Description | n/a |
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| Residue | 735 |
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| Sequence | MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPS
HFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVN
HPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHS
LGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHS
HSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRN
PANRLGSGPDGAEEIKRHVFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTP
KDSPGIPPSAGAHQLFRGFSFVATGLMEDDGKPRAPQAPLHSVVQQLHGKNLVFSDGYVV
KETIGVGSYSECKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYD
DGKHVYLVTELMRGGELLDKILRQKFFSEREASFVLHTIGKTVEYLHSQGVVHRDLKPSN
ILYVDESGNPECLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSL
GILLYTMLAGYTPFANGPSDTPEEILTRIGSGKFTLSGGNWNTVSETAKDLVSKMLHVDP
HQRLTAKQVLQHPWVTQKDKLPQSQLSHQDLQLVKGAMAATYSALNSSKPTPQLKPIESS
ILAQRRVRKLPSTTL
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| oxadiazole-containing compound, 10 |
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| Name | oxadiazole-containing compound, 10 |
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| Synonyms: | 4-[7-(3-aminopropoxy)-1-ethyl-4-phenyl-1H-imidazo[4,5-c]pyridin-2-yl]-1,2,5-oxadiazol-3-amine |
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| Type | Small organic molecule |
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| Emp. Form. | C19H21N7O2 |
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| Mol. Mass. | 379.4157 |
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| SMILES | CCn1c(nc2c(ncc(OCCCN)c12)-c1ccccc1)-c1nonc1N |
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| Structure | |
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| RSK1 Substrate Peptide |
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| Name | RSK1 Substrate Peptide |
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| Synonyms | n/a |
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| Type | Peptide |
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| Mol. Mass. | n/a |
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| Organism | n/a |
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| Description | n/a |
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| Residue | 11 |
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| Sequence | |
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