Target
Mitogen-activated protein kinase 14
Ligand
BDBM50314787
Substrate
n/a
Meas. Tech.
ChEMBL_627007 (CHEMBL1103663)
Ki
1.7±n/a nM
Citation
 Pettus, LHWurz, RPXu, SHerberich, BHenkle, BLiu, QMcBride, HJMu, SPlant, MHSaris, CJSherman, LWong, LMChmait, SLee, MRMohr, CHsieh, FTasker, AS Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase. J Med Chem 53:2973-85 (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:
BDBM50314787
Synonyms:
3-(1-(2,6-Difluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1Hpyrazolo[3,4-b]pyridin-5-yl)-4-methyl-N-(1-methylcyclopropyl)-benzamide | CHEMBL1092011
Type:
Small organic molecule
Emp. Form.:
C25H22F2N4O2
Mol. Mass.:
448.4646
SMILES:
Cc1ccc(cc1-c1cc2cnn(-c3c(F)cccc3F)c2n(C)c1=O)C(=O)NC1(C)CC1 |(-1.2,4.58,;.14,3.81,;1.47,4.59,;2.81,3.82,;2.81,2.28,;1.48,1.51,;.14,2.27,;-1.19,1.5,;-2.52,2.27,;-3.85,1.49,;-5.32,1.96,;-6.22,.71,;-5.29,-.54,;-6.06,-1.88,;-7.55,-1.96,;-8.33,-.61,;-8.31,-3.3,;-7.47,-4.59,;-5.93,-4.58,;-5.27,-3.23,;-3.69,-3.4,;-3.85,-.05,;-2.51,-.81,;-2.51,-2.35,;-1.18,-.04,;.15,-.81,;4.15,1.52,;4.15,-.02,;5.48,2.29,;6.81,1.52,;6.82,.02,;7.8,2.71,;8.33,1.26,)|
Structure:
Search PDB for entries with ligand similarity: