Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 14
Ligand
BDBM19438
Substrate
EGF receptor peptide
Meas. Tech.
p38 Enzyme Assay.
pH
7.5±n/a
Temperature
303.15±n/a K
IC50
62±n/a nM
Comments
LPS-induced TNF production in rat (rLPS), inhibition @ 20 mpk =89 %.
Citation
 Graneto, MJ; Kurumbail, RG; Vazquez, ML; Shieh, HS; Pawlitz, JL; Williams, JM; Stallings, WC; Geng, L; Naraian, AS; Koszyk, FJ; Stealey, MA; Xu, XD; Weier, RM; Hanson, GJ; Mourey, RJ; Compton, RP; Mnich, SJ; Anderson, GD; Monahan, JB; Devraj, R Synthesis, Crystal Structure, and Activity of Pyrazole-Based Inhibitors of p38 Kinase. J Med Chem 50:5712-9 (2007) [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:
BDBM19438
Synonyms:
4-{5-[(8aS)-octahydropyrrolo[1,2-a]piperazin-2-yl]-3-(4-chlorophenyl)-1H-pyrazol-4-yl}pyridine | Pyrazole-Based Inhibitor, 19
Type:
Small organic molecule
Emp. Form.:
C21H22ClN5
Mol. Mass.:
379.886
SMILES:
Clc1ccc(cc1)-c1n[nH]c(N2CCN3CCC[C@H]3C2)c1-c1ccncc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
EGF receptor peptide
Synonyms:
Epidermal Growth Factor Receptor Peptide (EGFRP)
Type:
Peptide
Mol. Mass.:
2318.63
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
KRELVEPLTPSGEAPNQALLR