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TargetMitogen-activated protein kinase 14
LigandBDBM50341365
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742454 (CHEMBL1769102)
IC50 6±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
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Mitogen-activated protein kinase 14
Name:Mitogen-activated protein kinase 14
Synonyms:CSAID-binding protein | CSBP | CSBP1 | CSBP2 | CSPB1 | Cytokine suppressive anti-inflammatory drug-binding protein | MAP kinase 14 | MAP kinase MXI2 | MAP kinase p38 alpha | MAPK 14 | MAPK14 | MAX-interacting protein 2 | MK14_HUMAN | MXI2 | Mitogen-activated protein kinase p38 alpha | SAPK2A | Stress-activated protein kinase 2a | p38 MAP kinase alpha/beta
Type:Serine/threonine-protein kinase
Mol. Mass.:41286.76
Organism:Homo sapiens (Human)
Description:Q16539
Residue:360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ
KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG
TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA
QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
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  Blast E-value cutoff:
BDBM50341365
n/a
NameBDBM50341365
Synonyms:6-(2,4-Difluorophenoxy)-8-(3-methanesulfonyl-propyl)-2-(tetrahydro-pyran-4-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one | CHEMBL1766502
TypeSmall organic molecule
Emp. Form.C22H24F2N4O5S
Mol. Mass.494.512
SMILESCS(=O)(=O)CCCn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure
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