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Target
Ribosomal protein S6 kinase alpha-1
Ligand
BDBM50585046
Substrate
n/a
Meas. Tech.
ChEMBL_2161428 (CHEMBL5046178)
IC50
82±n/a nM
Citation
 Powell, CE; Hatcher, JM; Jiang, J; Vatsan, PS; Che, J; Gray, NS Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett 13:577-585 (2022) [PubMed]  Article 
Target
Name:
Ribosomal protein S6 kinase alpha-1
Synonyms:
S6K-alpha 1 | RSK-1 | RPS6KA1(Kin.Dom.1 - N-terminal) | p90-RSK 1 | Ribosomal S6 kinase 1 (RSK1) | MAP kinase-activated protein kinase 1a | RPS6KA1(Kin.Dom.2 - C-terminal) | Ribosomal S6 kinase 1 | Ribosomal S6 Kinase 1 (RSK-1) | pp90RSK1 | Ribosomal protein S6 kinase alpha-1 | 90 kDa ribosomal protein S6 kinase 1 | p90S6K | Ribosomal protein S6 kinase alpha-1 (RSK1) | KS6A1_HUMAN | RPS6KA1 | MAPKAPK1A | RSK1 | p90RSK | Ribosomal protein S6 kinase alpha 1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
82736.10
Organism:
Human
Description:
n/a
Residue:
735
Sequence:
MPLAQLKEPWPLMELVPLDPENGQTSGEEAGLQPSKDEGVLKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDSGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHSHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHVFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTPKDSPGIPPSAGAHQLFRGFSFVATGLMEDDGKPRAPQAPLHSVVQQLHGKNLVFSDGYVVKETIGVGSYSECKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKHVYLVTELMRGGELLDKILRQKFFSEREASFVLHTIGKTVEYLHSQGVVHRDLKPSNILYVDESGNPECLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSLGILLYTMLAGYTPFANGPSDTPEEILTRIGSGKFTLSGGNWNTVSETAKDLVSKMLHVDPHQRLTAKQVLQHPWVTQKDKLPQSQLSHQDLQLVKGAMAATYSALNSSKPTPQLKPIESSILAQRRVRKLPSTTL
  
Inhibitor
Name:
BDBM50585046
Synonyms:
CHEMBL5086263
Type:
Small organic molecule
Emp. Form.:
C22H18F4N8O
Mol. Mass.:
486.43
SMILES:
CN1Cc2nn(C)c(C#N)c2-c2cnc3[nH]c(F)c(-c4cn(CCCC1=O)nc4C(F)(F)F)c3c2
Structure:
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