Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 14
Ligand
BDBM16520
Substrate
biotinylated GST-ATF2
Meas. Tech.
Enzyme Inhibition Scintillation Proximity Assay
pH
7±n/a
Temperature
303.15±n/a K
IC50
3500±n/a nM
Citation
 Natarajan, SR; Heller, ST; Nam, K; Singh, SB; Scapin, G; Patel, S; Thompson, JE; Fitzgerald, CE; O'Keefe, SJ p38 MAP kinase inhibitors. Part 6: 2-arylpyridazin-3-ones as templates for inhibitor design. Bioorg Med Chem Lett 16:5809-13 (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:
BDBM16520
Synonyms:
2-(2-chlorophenyl)-6-{[(2-methylphenyl)methyl]amino}-2,3-dihydropyridazin-3-one | 2-arylpyridazin-3-one, 25
Type:
Small organic molecule
Emp. Form.:
C18H16ClN3O
Mol. Mass.:
325.792
SMILES:
Cc1ccccc1CNc1ccc(=O)n(n1)-c1ccccc1Cl
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