Target
Mitogen-activated protein kinase 14 [G110D]
Ligand
BDBM15241
Substrate
biotinylated GST-ATF2
Meas. Tech.
Enzyme Inhibition Scintillation Proximity Assay
pH
7±n/a
Temperature
303.15±n/a K
IC50
67±n/a nM
Km
48000±4000 nM
Citation
 Fitzgerald, CEPatel, SBBecker, JWCameron, PMZaller, DPikounis, VBO'Keefe, SJScapin, G Structural basis for p38alpha MAP kinase quinazolinone and pyridol-pyrimidine inhibitor specificity. Nat Struct Biol 10:764-9 (2003) [PubMed]  Article 
Target
Name:
Mitogen-activated protein kinase 14 [G110D]
Synonyms:
Crk1 | Csbp1 | Csbp2 | MAP Kinase p38 alpha Mutant (G110D) | MK14_MOUSE | Mapk14 | Mitogen-activated protein kinase 14 | Mitogen-activated protein kinase p38 alpha
Type:
Enzyme
Mol. Mass.:
41338.25
Organism:
Mus musculus (mouse)
Description:
Mutant was site-directed generated from wild-type p38alpha.
Residue:
360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGHRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMDADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLAQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
  
Inhibitor
Name:
BDBM15241
Synonyms:
1-(2,6-dichlorophenyl)-5-(2,4-difluorophenyl)-7-(piperazin-1-yl)-1,2,3,4-tetrahydroquinazolin-2-one | 1-(2,6-dichlorophenyl)-5-(2,4-difluorophenyl)-7-piperazin-1-yl-3,4-dihydroquinazolin-2-one | CHEMBL94417 | quinazolinone compound 2
Type:
Small organic molecule
Emp. Form.:
C24H20Cl2F2N4O
Mol. Mass.:
489.345
SMILES:
Fc1ccc(c(F)c1)-c1cc(cc2N(C(=O)NCc12)c1c(Cl)cccc1Cl)N1CCNCC1
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