Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 14 [G110D]
Ligand
BDBM15243
Substrate
biotinylated GST-ATF2
Meas. Tech.
Enzyme Inhibition Scintillation Proximity Assay
pH
7±n/a
Temperature
303.15±n/a K
IC50
160±n/a nM
Km
48000±4000 nM
Citation
 Fitzgerald, CE; Patel, SB; Becker, JW; Cameron, PM; Zaller, D; Pikounis, VB; O'Keefe, SJ; Scapin, 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:
BDBM15243
Synonyms:
1-(2,6-dichlorophenyl)-6-[(2,4-difluorophenyl)sulfanyl]-7-(1,2,3,6-tetrahydropyridin-4-yl)-1H,2H,3H,4H-pyrido[3,2-d]pyrimidin-2-one | 10-(2,6-dichlorophenyl)-4-(2,4-difluorophenyl)sulfanyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-5,8,10-triazabicyclo[4.4.0]deca-2,4,7,11-tetraen-9-one | pyridol-pyrimidine compound 4
Type:
Small organic molecule
Emp. Form.:
C24H18Cl2F2N4OS
Mol. Mass.:
519.394
SMILES:
Fc1ccc(Sc2nc3CNC(=O)N(c3cc2C2=CCNCC2)c2c(Cl)cccc2Cl)c(F)c1 |t:19|
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