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Target
Ribosomal protein S6 kinase alpha-4
Ligand
BDBM50341342
Substrate
n/a
Meas. Tech.
ChEMBL_742527 (CHEMBL1769286)
Kd
73±n/a nM
Citation
 Goldstein, DM; Soth, M; Gabriel, T; Dewdney, N; Kuglstatter, A; Arzeno, H; Chen, J; Bingenheimer, W; Dalrymple, SA; Dunn, J; Farrell, R; Frauchiger, S; La Fargue, J; Ghate, M; Graves, B; Hill, RJ; Li, F; Litman, R; Loe, B; McIntosh, J; McWeeney, D; Papp, E; Park, J; Reese, HF; Roberts, RT; Rotstein, D; San Pablo, B; Sarma, K; Stahl, M; Sung, ML; Suttman, RT; Sjogren, EB; Tan, Y; Trejo, A; Welch, M; Weller, P; Wong, BR; Zecic, H Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors J Med Chem 54:2255-65 (2011) [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:
BDBM50341342
Synonyms:
6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1230122
Type:
Small organic molecule
Emp. Form.:
C19H18F2N4O3
Mol. Mass.:
388.368
SMILES:
Cn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure:
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