Target
Ribosomal protein S6 kinase alpha-1
Ligand
BDBM258595
Substrate
n/a
Meas. Tech.
Competition Binding Assay
Temperature
298.15±n/a K
IC50
5.01±n/a nM
Comments
extracted
Citation
 Akama, TJarnagin, KZhang, YZhou, YPlattner, JJSullivan, DC Boron-containing small molecules US Patent  US9493490 Publication Date 11/15/2016 
Target
Name:
Ribosomal protein S6 kinase alpha-1
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
Type:
Serine/threonine-protein kinase
Mol. Mass.:
82736.10
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
735
Sequence:
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTPKDSPGIPPSAGAHQLFRGFSFVATGLMEDDGKPRAPQAPLHSVVQQLHGKNLVFSDGYVVKETIGVGSYSECKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKHVYLVTELMRGGELLDKILRQKFFSEREASFVLHTIGKTVEYLHSQGVVHRDLKPSNILYVDESGNPECLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSLGILLYTMLAGYTPFANGPSDTPEEILTRIGSGKFTLSGGNWNTVSETAKDLVSKMLHVDPHQRLTAKQVLQHPWVTQKDKLPQSQLSHQDLQLVKGAMAATYSALNSSKPTPQLKPIESSILAQRRVRKLPSTTL
  
Inhibitor
Name:
BDBM258595
Synonyms:
US9493490, 6-(4-(aminomethyl)-2-fluorophenoxy)-7-methylbenzo[c][1,2]oxaborol-1(3H)-ol | US9493490, D | US9493490, Example 4
Type:
Small organic molecule
Emp. Form.:
C15H15BFNO3
Mol. Mass.:
287.094
SMILES:
Cc1c2B(O)OCc2ccc1Oc1ccc(CN)cc1F
Structure:
Search PDB for entries with ligand similarity: