Reaction Details  Report a problem with these data
Target
Mitogen-activated protein kinase 14
Ligand
BDBM17726
Substrate
biotinylated GST-ATF2
Meas. Tech.
HTRF Kinase Inhibition Assay
IC50
420±n/a nM
Citation
 Martin, MW; Newcomb, J; Nunes, JJ; McGowan, DC; Armistead, DM; Boucher, C; Buchanan, JL; Buckner, W; Chai, L; Elbaum, D; Epstein, LF; Faust, T; Flynn, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Lee, JH; Metz, D; Middleton, S; Mohn, D; Morgenstern, K; Morrison, MJ; Novak, PM; Oliveira-dos-Santos, A; Powers, D; Rose, P; Schneider, S; Sell, S; Tudor, Y; Turci, SM; Welcher, AA; White, RD; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Amouzegh, P; Ermann, M; Jenkins, J; Johnston, D; Napier, S; Power, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem 49:4981-91 (2006) [PubMed]  Article
Target
Name:
Mitogen-activated protein kinase 14
Synonyms:
CSAID-binding protein | CSBP | CSBP1 | CSBP2 | CSPB1 | Cytokine suppressive anti-inflammatory drug-binding protein | MAP kinase 14 | MAP kinase MXI2 | MAP kinase p38 alpha | MAPK 14 | MAPK14 | MAX-interacting protein 2 | MK14_HUMAN | MXI2 | Mitogen-activated protein kinase p38 alpha | SAPK2A | Stress-activated protein kinase 2a | p38 MAP kinase alpha/beta
Type:
Serine/threonine-protein kinase
Mol. Mass.:
41286.76
Organism:
Homo sapiens (Human)
Description:
Q16539
Residue:
360
Sequence:
MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQSIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQKLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMTGYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVGTPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAAQALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
  
Inhibitor
Name:
BDBM17726
Synonyms:
2,6-dimethylphenyl N-(2-methoxyphenyl)-N-(2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)carbamate | 2-aminopyrimidine carbamate, 25
Type:
Small organic molecule
Emp. Form.:
C31H34N6O3
Mol. Mass.:
538.6401
SMILES:
COc1ccccc1N(C(=O)Oc1c(C)cccc1C)c1ccnc(Nc2ccc(cc2)N2CCN(C)CC2)n1
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