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TargetMAP kinase p38
LigandBDBM50314070
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742456
Kd 1.3±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
 
MAP kinase p38
Name:MAP kinase p38
Synonyms:CSAID-binding protein | CSBP | Cytokine suppressive anti-inflammatory drug-binding protein | MAP Kinase p38 alpha | MAP kinase MXI2 | MAX-interacting protein 2 | Mitogen-activated protein kinase (MAP) p38 alpha | Mitogen-activated protein kinase (Map p38 alpha) | Mitogen-activated protein kinase 14 (MAP kinase p38 alpha) | Mitogen-activated protein kinase 14 (MAPK14 p38 alpha) | Mitogen-activated protein kinase 14 (MAPK14) | Mitogen-activated protein kinase 14 (MAPK14) (p38 MAPKα) | Mitogen-activated protein kinase 14 (MAPK14) (p38 MAPKa) | Mitogen-activated protein kinase 14 (p38 MAPKa) | Mitogen-activated protein kinase 14 (p38 alpha) | Mitogen-activated protein kinase 14, activated protein kinase p38 alpha | Mitogen-activated protein kinase p38 alpha | Mitogen-activated protein kinase p38 alpha (p38 MAPKa) | SAPK2A | p38-alpha
Type:Serine/threonine-protein kinase
Mol. Mass.:41286.76
Organism:Homo sapiens (human)
Description:n/a
Residue:360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ
KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG
TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA
QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
Blast this sequence in BindingDB or PDB
  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:
n/a