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Target
Mitogen-activated protein kinase 14
Ligand
BDBM50310984
Substrate
n/a
Meas. Tech.
ChEMBL_618897 (CHEMBL1101788)
IC50
59±n/a nM
Citation
Selness, SR; Devraj, RV; Monahan, JB; Boehm, TL; Walker, JK; Devadas, B; Durley, RC; Kurumbail, R; Shieh, H; Xing, L; Hepperle, M; Rucker, PV; Jerome, KD; Benson, AG; Marrufo, LD; Madsen, HM; Hitchcock, J; Owen, TJ; Christie, L; Promo, MA; Hickory, BS; Alvira, E; Naing, W; Blevis-Bal, R Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase. Bioorg Med Chem Lett 19:5851-6 (2009) [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:
BDBM50310984
Synonyms:
3-bromo-4-(2,4-difluorobenzyloxy)-1-(4-((dimethylamino)methyl)benzyl)-6-methylpyridin-2(1H)-one | CHEMBL1078665 | PHA-745052
Type:
Small organic molecule
Emp. Form.:
C23H23BrF2N2O2
Mol. Mass.:
477.342
SMILES:
CN(C)Cc1ccc(Cn2c(C)cc(OCc3ccc(F)cc3F)c(Br)c2=O)cc1