Reaction Details
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Mitogen-activated protein kinase 14
Ligand
BDBM14857
Substrate
BDBM10852
Meas. Tech.
Thermal Denaturation Assay
Kd
1.5±n/a nM
Citation
Regan, J; Capolino, A; Cirillo, PF; Gilmore, T; Graham, AG; Hickey, E; Kroe, RR; Madwed, J; Moriak, M; Nelson, R; Pargellis, CA; Swinamer, A; Torcellini, C; Tsang, M; Moss, 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 More Info.:
Target
Name:
Mitogen-activated protein kinase 14
Synonyms:
Crk1 | Csbp1 | Csbp2 | MAP Kinase p38 alpha | MAP kinase p38 | MK14_MOUSE | Mapk14 | 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:
BDBM14857
Synonyms:
1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-{4-[2-((2S,-6R)-2,6-dimethylmorpholin-4-yl)-ethoxy]naphthalen-1-yl}urea | 3-[3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-yl]-1-(4-{2-[(2R,6S)-2,6-dimethylmorpholin-4-yl]ethoxy}naphthalen-1-yl)urea | BIRB-796 Analog 45
Type:
Small organic molecule
Emp. Form.:
C33H41N5O3
Mol. Mass.:
555.7103
SMILES:
C[C@H]1CN(CCOc2ccc(NC(=O)Nc3cc(nn3-c3ccc(C)cc3)C(C)(C)C)c3ccccc23)C[C@@H](C)O1 |r|
Structure:
Substrate