Target
Mitogen-activated protein kinase 14
Ligand
BDBM50327007
Substrate
n/a
Meas. Tech.
ChEMBL_663513 (CHEMBL1251166)
IC50
222±n/a nM
Citation
 Liu, CLin, JWrobleski, STLin, SHynes, JWu, HDyckman, AJLi, TWityak, JGillooly, KMPitt, SShen, DRZhang, RFMcIntyre, KWSalter-Cid, LShuster, DJZhang, HMarathe, PHDoweyko, AMSack, JSKiefer, SEKish, KFNewitt, JAMcKinnon, MDodd, JHBarrish, JCSchieven, GLLeftheris, K Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases. J Med Chem 53:6629-39 (2010) [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:
BDBM50327007
Synonyms:
4-(5-(Cyclobutylcarbamoyl)-2-methylphenylamino)-N-ethyl-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide | CHEMBL1254503
Type:
Small organic molecule
Emp. Form.:
C22H26N6O2
Mol. Mass.:
406.4808
SMILES:
CCNC(=O)c1cn2ncnc(Nc3cc(ccc3C)C(=O)NC3CCC3)c2c1C
Structure:
Search PDB for entries with ligand similarity: