Reaction Details Report a problem with these data
Target
Mitogen-activated protein kinase 14
Ligand
BDBM50314786
Substrate
n/a
Meas. Tech.
ChEMBL_627007 (CHEMBL1103663)
Ki
1.5±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
More Info.:
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:
BDBM50314786
Synonyms:
3-(1-(2,6-Difluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1Hpyrazolo[3,4-b]pyridin-5-yl)-4-methylbenzamide | CHEMBL1091930
Type:
Small organic molecule
Emp. Form.:
C21H16F2N4O2
Mol. Mass.:
394.3741
SMILES:
Cc1ccc(cc1-c1cc2cnn(-c3c(F)cccc3F)c2n(C)c1=O)C(N)=O |(-.24,-4.57,;-1.57,-3.81,;-2.91,-4.58,;-4.24,-3.81,;-4.24,-2.27,;-2.91,-1.5,;-1.57,-2.27,;-.24,-1.49,;1.09,-2.26,;2.43,-1.49,;3.89,-1.97,;4.8,-.72,;3.87,.54,;4.64,1.87,;6.13,1.95,;6.91,.6,;6.9,3.28,;6.06,4.58,;4.52,4.58,;3.85,3.22,;2.27,3.4,;2.43,.05,;1.09,.82,;1.09,2.36,;-.24,.05,;-1.58,.81,;-5.58,-1.5,;-5.58,.04,;-6.91,-2.27,)|