| Reaction Details |
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 | Report a problem with these data |
| Target | Ribosomal protein S6 kinase alpha-1 |
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| Ligand | BDBM4814 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_776795 (CHEMBL1913892) |
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| IC50 | 131±n/a nM |
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| Citation |  Andreani, A; Granaiola, M; Leoni, A; Locatelli, A; Morigi, R; Rambaldi, M; Varoli, L; Lannigan, D; Smith, J; Scudiero, D; Kondapaka, S; Shoemaker, RH Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors. Eur J Med Chem46:4311-23 (2011) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Ribosomal protein S6 kinase alpha-1 |
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| Name: | Ribosomal protein S6 kinase alpha-1 |
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| Synonyms: | 90 kDa ribosomal protein S6 kinase 1 | KS6A1_HUMAN | MAP kinase-activated protein kinase 1a | MAPKAPK1A | RPS6KA1 | RPS6KA1(Kin.Dom.1 - N-terminal) | RPS6KA1(Kin.Dom.2 - C-terminal) | RSK-1 | RSK1 | Ribosomal S6 Kinase 1 (RSK-1) | Ribosomal S6 kinase 1 | Ribosomal S6 kinase 1 (RSK1) | Ribosomal protein S6 kinase alpha 1 | Ribosomal protein S6 kinase alpha-1 | Ribosomal protein S6 kinase alpha-1 (RSK1) | S6K-alpha 1 | p90-RSK 1 | p90RSK | p90S6K | pp90RSK1 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 82736.10 |
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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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| BDBM4814 |
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| n/a |
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| Name | BDBM4814 |
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| Synonyms: | CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide | SU11248 | SUNITINIB | SUNITINIB MALATE | US10464902, Sunitinib | US9163010, Sunitinib | US9914707, SU11248 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H27FN4O2 |
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| Mol. Mass. | 398.4738 |
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| SMILES | CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C |
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| Structure | 
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