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TargetRibosomal protein S6 kinase alpha-3
LigandBDBM50021670
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1368329 (CHEMBL868675)
IC50 410±n/a nM
Citation Costales, AMathur, MRamurthy, SLan, JSubramanian, SJain, RAtallah, GSetti, LLindvall, MAppleton, BAOrnelas, EFeucht, PWarne, BDoyle, LBasham, SEAronchik, IJefferson, ABShafer, 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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BDBM50021670
n/a
NameBDBM50021670
Synonyms:CHEMBL3297840
TypeSmall organic molecule
Emp. Form.C21H17FN2O3
Mol. Mass.364.3697
SMILESCOc1cccc(Nc2nc3cccc(-c4c(F)cccc4OC)c3o2)c1 |(6.37,-11.94,;7.13,-10.6,;6.36,-9.27,;4.81,-9.27,;4.04,-7.94,;4.82,-6.6,;6.36,-6.61,;7.13,-5.28,;8.67,-5.28,;9.58,-4.03,;11.04,-4.51,;12.37,-3.74,;13.71,-4.5,;13.71,-6.05,;12.38,-6.82,;12.37,-8.36,;11.04,-9.13,;9.71,-8.36,;11.04,-10.67,;12.37,-11.44,;13.71,-10.66,;13.71,-9.13,;15.04,-8.35,;16.38,-9.11,;11.04,-6.05,;9.57,-6.53,;7.13,-7.94,)|
Structure
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