Target
Mitogen-activated protein kinase 14
Ligand
BDBM14844
Substrate
BDBM10852
Meas. Tech.
Thermal Denaturation Assay
pH
7±n/a
Temperature
298.15±n/a K
Kd
0.18±.03 nM
Comments
Tm=61.3 C (apo-p38 Tm=46.6 C).
Citation
 Regan, JCapolino, ACirillo, PFGilmore, TGraham, AGHickey, EKroe, RRMadwed, JMoriak, MNelson, RPargellis, CASwinamer, ATorcellini, CTsang, MMoss, N Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796). J Med Chem 46:4676-86 (2003) [PubMed]  Article
Target
Name:
Mitogen-activated protein kinase 14
Synonyms:
CRK1 | MAP Kinase p38 alpha | MAP kinase p38 | Mitogen-activated protein kinase 14 | Mitogen-activated protein kinase p38 alpha
Type:
Enzyme
Mol. Mass.:
41281.22
Organism:
Mus musculus (mouse)
Description:
The full-length open reading frame of murine p38 alpha was cloned and expressed in E. coli.. Soluble murine p38R was extracted from cell pellets and purified using ion-exchange chromatography.
Residue:
360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGHRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLAQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
  
Inhibitor
Name:
BDBM14844
Synonyms:
1-[5-tert-Butyl-2-(6-methyl-pyridin-3-yl)-2H-pyrazol-3-yl]-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea | 3-[3-tert-butyl-1-(6-methylpyridin-3-yl)-1H-pyrazol-5-yl]-1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}urea | BIRB-796 Analog 17 | CHEMBL104991
Type:
Small organic molecule
Emp. Form.:
C30H36N6O3
Mol. Mass.:
528.6452
SMILES:
Cc1ccc(cn1)-n1nc(cc1NC(=O)Nc1ccc(OCCN2CCOCC2)c2ccccc12)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate