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Target
Mitogen-activated protein kinase 14
Ligand
BDBM17064
Substrate
biotinylated GST-ATF2
Meas. Tech.
Enzyme Inhibition Scintillation Proximity Assay
pH
7±n/a
Temperature
303.15±n/a K
IC50
5.3±n/a nM
Citation
 Natarajan, SR; Wisnoski, DD; Thompson, JE; O'Neill, EA; O'Keefe, SJ p38 MAP kinase inhibitors. Part 3: SAR on 3,4-dihydropyrimido[4,5-d]pyrimidin-2-ones and 3,4-dihydropyrido[4,3-d]pyrimidin-2-ones. Bioorg Med Chem Lett 16:4400-4 (2006) [PubMed]  Article 
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:
BDBM17064
Synonyms:
7-amino-5-(2-chlorophenyl)-1-(2,6-dichlorophenyl)-1H,2H,3H,4H-[1,3]diazino[4,5-d]pyrimidin-2-one | pyrimido-pyrimidine, 24
Type:
Small organic molecule
Emp. Form.:
C18H12Cl3N5O
Mol. Mass.:
420.68
SMILES:
Nc1nc2N(C(=O)NCc2c(n1)-c1ccccc1Cl)c1c(Cl)cccc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated GST-ATF2
Synonyms:
ATF-2-GST | ATF2 | Activating transcription factor 2 | Activating transcription factor 2-GST fusion | GST-ATF2 | biotinylated ATF2 substrate | biotinylated activating transcription factor 2
Type:
Other Protein Type
Mol. Mass.:
12237.77
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
109
Sequence:
MSDDKPFLCTAPGCGQRFTNEDHLAVHKHKHEMTLKFGPARNDSVIVADQTPTPTRFLKNCEEVGLFNELASPFENEFKKASEDDIKKMPLDLSPLATPIIRSKIEEPS