Target
Mitogen-activated protein kinase 14
Ligand
BDBM50341368
Substrate
n/a
Meas. Tech.
ChEMBL_742454 (CHEMBL1769102)
IC50
7±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 Chem 54:2255-65 (2011) [PubMed]  Article 
Target
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:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
  
Inhibitor
Name:
BDBM50341368
Synonyms:
6-(2,4-Difluorophenoxy)-8-((S)-2,3-dihydroxy-propyl)-2-(tetrahydro-pyran-4-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one | CHEMBL1766505
Type:
Small organic molecule
Emp. Form.:
C21H22F2N4O5
Mol. Mass.:
448.42
SMILES:
OC[C@@H](O)Cn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O |r|
Structure:
Search PDB for entries with ligand similarity: