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Target
Ribosomal protein S6 kinase alpha-4
Ligand
BDBM50601138
Substrate
n/a
Meas. Tech.
ChEMBL_2235868 (CHEMBL5149640)
IC50
20±n/a nM
Citation
 Hall, A; Abendroth, J; Bolejack, MJ; Ceska, T; Dell'Aiera, S; Ellis, V; Fox, D; François, C; Muruthi, MM; Prével, C; Poullennec, K; Romanov, S; Valade, A; Vanbellinghen, A; Yano, J; Geraerts, M Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. ACS Med Chem Lett 13:1099-1108 (2022) [PubMed] 
Target
Name:
Ribosomal protein S6 kinase alpha-4
Synonyms:
90 kDa ribosomal protein S6 kinase 4 | KS6A4_HUMAN | MSK2 | Mitogen- and Stress-Activated Protein Kinase 2 (MSK2) | Nuclear mitogen- and stress-activated protein kinase 2 | RPS6KA4 | RPS6KA4(Kin.Dom.1 - N-terminal) | RSKB | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha 4 | Ribosomal protein S6 kinase alpha-4 | Ribosomal protein kinase B
Type:
Serine/threonine-protein kinase
Mol. Mass.:
85620.38
Organism:
Homo sapiens (Human)
Description:
Recombinant MSK2 was phosphorylated by incubation with active p38alpha before assays.
Residue:
772
Sequence:
MGDEDDDESCAVELRITEANLTGHEEKVSVENFELLKVLGTGAYGKVFLVRKAGGHDAGKLYAMKVLRKAALVQRAKTQEHTRTERSVLELVRQAPFLVTLHYAFQTDAKLHLILDYVSGGEMFTHLYQRQYFKEAEVRVYGGEIVLALEHLHKLGIIYRDLKLENVLLDSEGHIVLTDFGLSKEFLTEEKERTFSFCGTIEYMAPEIIRSKTGHGKAVDWWSLGILLFELLTGASPFTLEGERNTQAEVSRRILKCSPPFPPRIGPVAQDLLQRLLCKDPKKRLGAGPQGAQEVRNHPFFQGLDWVALAARKIPAPFRPQIRSELDVGNFAEEFTRLEPVYSPPGSPPPGDPRIFQGYSFVAPSILFDHNNAVMTDGLEAPGAGDRPGRAAVARSAMMQDSPFFQQYELDLREPALGQGSFSVCRRCRQRQSGQEFAVKILSRRLEANTQREVAALRLCQSHPNVVNLHEVHHDQLHTYLVLELLRGGELLEHIRKKRHFSESEASQILRSLVSAVSFMHEEAGVVHRDLKPENILYADDTPGAPVKIIDFGFARLRPQSPGVPMQTPCFTLQYAAPELLAQQGYDESCDLWSLGVILYMMLSGQVPFQGASGQGGQSQAAEIMCKIREGRFSLDGEAWQGVSEEAKELVRGLLTVDPAKRLKLEGLRGSSWLQDGSARSSPPLRTPDVLESSGPAVRSGLNATFMAFNRGKREGFFLKSVENAPLAKRRKQKLRSATASRRGSPAPANPGRAPVASKGAPRRANGPLPPS
  
Inhibitor
Name:
BDBM50601138
Synonyms:
CHEMBL5184056
Type:
Small organic molecule
Emp. Form.:
C12H6ClN5
Mol. Mass.:
255.663
SMILES:
Clc1ccc(C#N)c(n1)-n1ccc2ncncc12
Structure:
Search PDB for entries with ligand similarity: