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TargetRibosomal protein S6 kinase alpha 4
LigandBDBM50314070
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742527
Kd 150±n/a nM
Citation Goldstein, DMSoth, MGabriel, TDewdney, NKuglstatter, AArzeno, HChen, JBingenheimer, WDalrymple, SADunn, JFarrell, RFrauchiger, SLa Fargue, JGhate, MGraves, BHill, RJLi, FLitman, RLoe, BMcIntosh, JMcWeeney, DPapp, EPark, JReese, HFRoberts, RTRotstein, DSan Pablo, BSarma, KStahl, MSung, MLSuttman, RTSjogren, EBTan, YTrejo, AWelch, MWeller, PWong, BRZecic, 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 Chem54:2255-65 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Ribosomal protein S6 kinase alpha 4
Name:Ribosomal protein S6 kinase alpha 4
Synonyms:90 kDa ribosomal protein S6 kinase 4 | Mitogen- and Stress-Activated Protein Kinase 2 (MSK2) | Nuclear mitogen- and stress-activated protein kinase 2 | RSKB | 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:
MGDEDDDESCAVELRITEANLTGHEEKVSVENFELLKVLGTGAYGKVFLVRKAGGHDAGK
LYAMKVLRKAALVQRAKTQEHTRTERSVLELVRQAPFLVTLHYAFQTDAKLHLILDYVSG
GEMFTHLYQRQYFKEAEVRVYGGEIVLALEHLHKLGIIYRDLKLENVLLDSEGHIVLTDF
GLSKEFLTEEKERTFSFCGTIEYMAPEIIRSKTGHGKAVDWWSLGILLFELLTGASPFTL
EGERNTQAEVSRRILKCSPPFPPRIGPVAQDLLQRLLCKDPKKRLGAGPQGAQEVRNHPF
FQGLDWVALAARKIPAPFRPQIRSELDVGNFAEEFTRLEPVYSPPGSPPPGDPRIFQGYS
FVAPSILFDHNNAVMTDGLEAPGAGDRPGRAAVARSAMMQDSPFFQQYELDLREPALGQG
SFSVCRRCRQRQSGQEFAVKILSRRLEANTQREVAALRLCQSHPNVVNLHEVHHDQLHTY
LVLELLRGGELLEHIRKKRHFSESEASQILRSLVSAVSFMHEEAGVVHRDLKPENILYAD
DTPGAPVKIIDFGFARLRPQSPGVPMQTPCFTLQYAAPELLAQQGYDESCDLWSLGVILY
MMLSGQVPFQGASGQGGQSQAAEIMCKIREGRFSLDGEAWQGVSEEAKELVRGLLTVDPA
KRLKLEGLRGSSWLQDGSARSSPPLRTPDVLESSGPAVRSGLNATFMAFNRGKREGFFLK
SVENAPLAKRRKQKLRSATASRRGSPAPANPGRAPVASKGAPRRANGPLPPS
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  Blast E-value cutoff:
BDBM50314070
NameBDBM50314070
Synonyms:6-(2,4-difluorophenoxy)-2-{[3-hydroxy-1-(2-hydroxyethyl)propyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1090089 | pamapimod
TypeSmall organic molecule
Emp. Form.C19H20F2N4O4
Mol. Mass.406.3833
SMILESCn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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