Reaction Details Report a problem with these data
Target
Ribosomal protein S6 kinase alpha-1 [E551G,S637N,G697A]
Ligand
BDBM25017
Substrate
RSK Substrate Peptide
Meas. Tech.
Kinase Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
31±5 nM
Citation
 Sapkota, GP; Cummings, L; Newell, FS; Armstrong, C; Bain, J; Frodin, M; Grauert, M; Hoffmann, M; Schnapp, G; Steegmaier, M; Cohen, P; Alessi, DR BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem J 401:29-38 (2007) [PubMed]  Article 
Target
Name:
Ribosomal protein S6 kinase alpha-1 [E551G,S637N,G697A]
Synonyms:
90 kDa ribosomal protein S6 kinase 1 | KS6A1_RAT | MAP kinase-activated protein kinase 1a | Mapkapk1a | Ribosomal S6 Kinase 1 (RSK-1) | Ribosomal protein S6 kinase alpha-1 | Rps6ka1 | Rsk1 | p90-RSK 1 | p90S6K | pp90RSK1
Type:
Serine/threonine-protein kinase
Mol. Mass.:
82866.82
Organism:
Rattus norvegicus (rat)
Description:
The rat RSK1 sequence contained His6-tag positioned N-terminal to the initiating methionine residue and differed from the Genbank entry M99169, at three residues E551G, S637N and G697A. The protein was cloned and purified from baculovirus expression system.
Residue:
735
Sequence:
MPLAQLKEPWPLMELVPLDPENGQASGEEAGLQPSKDEGILKEISITHHVKAGSEKADPSHFELLKVLGQGSFGKVFLVRKVTRPDNGHLYAMKVLKKATLKVRDRVRTKMERDILADVNHPFVVKLHYAFQTEGKLYLILDFLRGGDLFTRLSKEVMFTEEDVKFYLAELALGLDHLHSLGIIYRDLKPENILLDEEGHIKLTDFGLSKEAIDHEKKAYSFCGTVEYMAPEVVNRQGHTHSADWWSYGVLMFEMLTGSLPFQGKDRKETMTLILKAKLGMPQFLSTEAQSLLRALFKRNPANRLGSGPDGAEEIKRHIFYSTIDWNKLYRREIKPPFKPAVAQPDDTFYFDTEFTSRTPRDSPGIPPSAGAHQLFRGFSFVATGLMEDDSKPRATQAPLHSVVQQLHGKNLVFSDGYIVKETIGVGSYSVCKRCVHKATNMEYAVKVIDKSKRDPSEEIEILLRYGQHPNIITLKDVYDDSKHVYLVTELMRGGELLDKILRQKFFSEREASFVLYTISKTVEYLHSQGVVHRDLKPSNILYVDESGNPGCLRICDFGFAKQLRAENGLLMTPCYTANFVAPEVLKRQGYDEGCDIWSLGVLLYTMLAGYTPFANGPSDTPEEILTRISSGKFTLNGGNWNTVSETAKDLVSKMLHVDPHQRLTAKQVLQHPWITQKDKLPQSQLSHQDLQLVKGAMAATYSALSSSKPTPQLKPIESSILAQRRVRKLPSTTL
  
Inhibitor
Name:
BDBM25017
Synonyms:
2-[(3,5-difluoro-4-hydroxyphenyl)amino]-5,7-dimethyl-8-(3-methylbutyl)-5,6,7,8-tetrahydropteridin-6-one | BI-D1870 | US11851436, Compound BI-D1870
Type:
Small organic molecule
Emp. Form.:
C19H23F2N5O2
Mol. Mass.:
391.415
SMILES:
CC(C)CCN1C(C)C(=O)N(C)c2cnc(Nc3cc(F)c(O)c(F)c3)nc12
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
RSK Substrate Peptide
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
1132.38
Organism:
n/a
Description:
n/a
Residue:
10
Sequence:
KKLNRTLSVA