Reaction Details
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Mitogen-activated protein kinase 14
Ligand
BDBM14842
Substrate
BDBM10852
Meas. Tech.
UV-Thermal Melt
pH
7±n/a
Temperature
298.15±n/a K
Kd
2400±640 nM
Comments
Tm=49.1 C (apo-p38 Tm=46.6 C).
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:
BDBM14842
Synonyms:
1-[4-(2-Morpholin-4-yl-ethoxy)-naphthalen-1-yl]-3-(2-phenyl-2H-pyrazol-3-yl)-urea | 1-{4-[2-(morpholin-4-yl)ethoxy]naphthalen-1-yl}-3-(1-phenyl-1H-pyrazol-5-yl)urea | BIRB-796 Analog 31 | CHEMBL104119 | Dopamine D2 receptor and serotonin 2a receptor | diaryl urea compound 1
Type:
Small organic molecule
Emp. Form.:
C26H27N5O3
Mol. Mass.:
457.5243
SMILES:
O=C(Nc1ccnn1-c1ccccc1)Nc1ccc(OCCN2CCOCC2)c2ccccc12
Structure:
Substrate