Target
Mitogen-activated protein kinase 14
Ligand
BDBM14835
Substrate
BDBM10852
Meas. Tech.
UV-Thermal Melt
pH
7±n/a
Temperature
298.15±n/a K
Kd
26±30 nM
Comments
Tm=54.5 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:
BDBM14835
Synonyms:
1-(5-tert-Butyl-2-methyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea | 3-(3-tert-butyl-1-methyl-1H-pyrazol-5-yl)-1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}urea | BIRB-796 Analog 35 | CHEMBL104749 | Dopamine D2 receptor and serotonin 2a receptor | diaryl urea compound 4
Type:
Small organic molecule
Emp. Form.:
C25H33N5O3
Mol. Mass.:
451.5612
SMILES:
Cn1nc(cc1NC(=O)Nc1ccc(OCCN2CCOCC2)c2ccccc12)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity:
Substrate