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Target
Mitogen-activated protein kinase 14
Ligand
BDBM50314785
Substrate
n/a
Meas. Tech.
ChEMBL_627007 (CHEMBL1103663)
Ki
0.8±n/a nM
Citation
 Pettus, LH; Wurz, RP; Xu, S; Herberich, B; Henkle, B; Liu, Q; McBride, HJ; Mu, S; Plant, MH; Saris, CJ; Sherman, L; Wong, LM; Chmait, S; Lee, MR; Mohr, C; Hsieh, F; Tasker, 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:
BDBM50314785
Synonyms:
CHEMBL1091929 | N-Cyclopropyl-3-(1-(2,6-difluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridin-5-yl)-5-fluoro-4-methylbenzamide
Type:
Small organic molecule
Emp. Form.:
C24H19F3N4O2
Mol. Mass.:
452.4285
SMILES:
Cc1c(F)cc(cc1-c1cc2cnn(-c3c(F)cccc3F)c2n(C)c1=O)C(=O)NC1CC1 |(1.2,-3.81,;-.13,-3.04,;-1.47,-3.81,;-1.46,-5.35,;-2.8,-3.04,;-2.8,-1.5,;-1.47,-.73,;-.14,-1.5,;1.2,-.73,;2.53,-1.49,;3.86,-.72,;5.33,-1.2,;6.23,.05,;5.3,1.31,;6.07,2.64,;7.56,2.72,;8.35,1.37,;8.33,4.06,;7.49,5.35,;5.95,5.35,;5.29,3.99,;3.7,4.17,;3.86,.82,;2.53,1.59,;2.53,3.13,;1.19,.81,;-.14,1.58,;-4.14,-.73,;-4.14,.81,;-5.47,-1.51,;-6.81,-.74,;-8.35,-.74,;-7.58,.6,)|
Structure:
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