Target
Ribosomal protein S6 kinase alpha-2
Ligand
BDBM50585046
Substrate
n/a
Meas. Tech.
ChEMBL_2161430 (CHEMBL5046180)
IC50
61±n/a nM
Citation
 Powell, CEHatcher, JMJiang, JVatsan, PSChe, JGray, NS Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett 13:577-585 (2022) [PubMed]  Article 
Target
Name:
Ribosomal protein S6 kinase alpha-2
Synonyms:
Ribosomal protein S6 kinase alpha-2 | 90 kDa ribosomal protein S6 kinase 2 | p90-RSK 2 | RPS6KA2(Kin.Dom.1 - N-terminal) | Ribosomal S6 Kinase 3 (RSK-3) | pp90RSK3 | MAP kinase-activated protein kinase 1c | 90 kDa ribosomal protein S6 kinase 2 (RSK2) | KS6A2_HUMAN | RPS6KA2 | MAPKAPK1C | RSK3 | p90RSK | Ribosomal protein S6 kinase alpha 2 (RSK2) | Ribosomal protein S6 kinase alpha 2
Type:
Serine/threonine-protein kinase
Mol. Mass.:
83259.46
Organism:
Human
Description:
n/a
Residue:
733
Sequence:
MDLSMKKFAVRRFFSVYLRRKSRSKSSSLSRLEEEGVVKEIDISHHVKEGFEKADPSQFELLKVLGQGSYGKVFLVRKVKGSDAGQLYAMKVLKKATLKVRDRVRSKMERDILAEVNHPFIVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALALDHLHSLGIIYRDLKPENILLDEEGHIKITDFGLSKEAIDHDKRAYSFCGTIEYMAPEVVNRRGHTQSADWWSFGVLMFEMLTGSLPFQGKDRKETMALILKAKLGMPQFLSGEAQSLLRALFKRNPCNRLGAGIDGVEEIKRHPFFVTIDWNTLYRKEIKPPFKPAVGRPEDTFHFDPEFTARTPTDSPGVPPSANAHHLFRGFSFVASSLIQEPSQQDLHKVPVHPIVQQLHGNNIHFTDGYEIKEDIGVGSYSVCKRCVHKATDTEYAVKIIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDGKFVYLVMELMRGGELLDRILRQRYFSEREASDVLCTITKTMDYLHSQGVVHRDLKPSNILYRDESGSPESIRVCDFGFAKQLRAGNGLLMTPCYTANFVAPEVLKRQGYDAACDIWSLGILLYTMLAGFTPFANGPDDTPEEILARIGSGKYALSGGNWDSISDAAKDVVSKMLHVDPHQRLTAMQVLKHPWVVNREYLSPNQLSRQDVHLVKGAMAATYFALNRTPQAPRLEPVLSSNLAQRRGMKRLTSTRL
  
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:
Search PDB for entries with ligand similarity: