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TargetMAP kinase p38
LigandBDBM50341342
Substrate/Competitorn/a
Meas. Tech.ChEMBL_742470
Kd 29±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
More Info.:Get all data from this article,  Assay Method
 
MAP kinase p38
Name:MAP kinase p38
Synonyms:MAP kinase p38 | Mitogen-activated protein kinase 11 | Mitogen-activated protein kinase p38 beta | Stress-activated protein kinase 2 | p38-2 | p38-beta | p38b
Type:Enzyme Catalytic Domain
Mol. Mass.:41351.73
Organism:Homo sapiens (Human)
Description:gi_20128774
Residue:364
Sequence:
MSGPRAGFYRQELNKTVWEVPQRLQGLRPVGSGAYGSVCSAYDARLRQKVAVKKLSRPFQ
SLIHARRTYRELRLLKHLKHENVIGLLDVFTPATSIEDFSEVYLVTTLMGADLNNIVKCQ
ALSDEHVQFLVYQLLRGLKYIHSAGIIHRDLKPSNVAVNEDCELRILDFGLARQADEEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLQGKALFPGSDYIDQLKRIMEVVG
TPSPEVLAKISSEHARTYIQSLPPMPQKDLSSIFRGANPLAIDLLGRMLVLDSDQRVSAA
EALAHAYFSQYHDPEDEPEAEPYDESVEAKERTLEEWKELTYQEVLSFKPPEPPKPPGSL
EIEQ
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50341342
n/a
NameBDBM50341342
Synonyms:6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1230122
TypeSmall organic molecule
Emp. Form.C19H18F2N4O3
Mol. Mass.388.368
SMILESCn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
Structure
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