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TargetRibosomal protein S6 kinase alpha-3
LigandBDBM50021671
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1368329 (CHEMBL868675)
IC50 490±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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BDBM50021671
n/a
NameBDBM50021671
Synonyms:CHEMBL3298042
TypeSmall organic molecule
Emp. Form.C24H23FN2O5
Mol. Mass.438.4482
SMILESCCOc1cccc(F)c1-c1cccc2nc(Nc3cc(OC)c(OC)c(OC)c3)oc12 |(22.28,-22.22,;20.95,-23,;19.61,-22.24,;18.28,-23.01,;18.29,-24.55,;16.95,-25.33,;15.61,-24.55,;15.61,-23.01,;14.28,-22.24,;16.95,-22.25,;16.94,-20.71,;18.28,-19.93,;18.27,-18.38,;16.94,-17.62,;15.61,-18.39,;14.15,-17.92,;13.24,-19.16,;11.7,-19.16,;10.93,-20.49,;11.7,-21.82,;10.93,-23.15,;11.7,-24.48,;10.94,-25.82,;9.38,-23.15,;8.61,-24.48,;7.07,-24.48,;8.61,-21.81,;7.07,-21.81,;6.31,-20.48,;9.39,-20.48,;14.14,-20.4,;15.61,-19.93,)|
Structure
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