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Target
Ribosomal protein S6 kinase alpha-4
Ligand
BDBM50308060
Substrate
n/a
Meas. Tech.
ChEMBL_655920 (CHEMBL1244964)
Kd
28±n/a nM
Citation
 Zarrinkar, PP; Gunawardane, RN; Cramer, MD; Gardner, MF; Brigham, D; Belli, B; Karaman, MW; Pratz, KW; Pallares, G; Chao, Q; Sprankle, KG; Patel, HK; Levis, M; Armstrong, RC; James, J; Bhagwat, SS AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood 114:2984-92 (2009) [PubMed]  Article 
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:
BDBM50308060
Synonyms:
16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one | CEP-701 | CHEMBL603469 | US11370779, Compound CEP-701
Type:
Small organic molecule
Emp. Form.:
C26H21N3O4
Mol. Mass.:
439.4626
SMILES:
C[C@]12O[C@H](C[C@]1(O)CO)n1c3ccccc3c3c4C(=O)NCc4c4c5ccccc5n2c4c13 |r|
Structure:
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