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TargetRibosomal protein S6 kinase alpha-3
LigandBDBM50021659
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1368328 (CHEMBL868674)
IC50 6300±n/a nM
Citation Costales, A; Mathur, M; Ramurthy, S; Lan, J; Subramanian, S; Jain, R; Atallah, G; Setti, L; Lindvall, M; Appleton, BA; Ornelas, E; Feucht, P; Warne, B; Doyle, L; Basham, SE; Aronchik, I; Jefferson, AB; Shafer, CM 2-Amino-7-substituted benzoxazole analogs as potent RSK2 inhibitors. Bioorg Med Chem Lett24:1592-6 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Ribosomal protein S6 kinase alpha-3
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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  Blast E-value cutoff:
BDBM50021659
n/a
NameBDBM50021659
Synonyms:CHEMBL3297951
TypeSmall organic molecule
Emp. Form.C25H24FN3O4
Mol. Mass.449.4742
SMILESCOc1ccc(Nc2nc3cccc(-c4c(F)cccc4OC)c3o2)cc1O[C@H]1CCNC1 |r,wU:28.31,(10.88,-23.43,;12.42,-23.43,;13.19,-22.09,;12.42,-20.76,;13.19,-19.42,;14.73,-19.43,;15.5,-18.1,;17.04,-18.1,;17.95,-16.86,;19.41,-17.33,;20.74,-16.56,;22.07,-17.32,;22.08,-18.87,;20.74,-19.65,;20.75,-21.19,;19.42,-21.96,;18.08,-21.18,;19.42,-23.49,;20.75,-24.27,;22.09,-23.49,;22.08,-21.95,;23.41,-21.18,;24.75,-21.94,;19.41,-18.87,;17.94,-19.35,;15.5,-20.76,;14.73,-22.09,;15.51,-23.42,;14.74,-24.76,;15.37,-26.16,;14.23,-27.2,;12.89,-26.43,;13.21,-24.92,)|
Structure
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