Target
Mitogen-activated protein kinase 14
Ligand
BDBM50296663
Substrate
n/a
Meas. Tech.
ChEMBL_582351 (CHEMBL1053415)
IC50
1.4±n/a nM
Citation
 Wurz, RPPettus, LHXu, SHenkle, BSherman, LPlant, MMiner, KMcBride, HWong, LMSaris, CJLee, MRChmait, SMohr, CHsieh, FTasker, AS Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase. Bioorg Med Chem Lett 19:4724-8 (2009) [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:
BDBM50296663
Synonyms:
CHEMBL560730 | N-cyclopropyl-3-(1-(2,6-difluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-4-methylbenzamide
Type:
Small organic molecule
Emp. Form.:
C24H20F2N4O3
Mol. Mass.:
450.4374
SMILES:
Cc1ccc(cc1Oc1cc(=O)n(C)c2n(ncc12)-c1c(F)cccc1F)C(=O)NC1CC1 |(-3.38,3.72,;-2.05,2.95,;-.72,3.72,;.62,2.95,;.62,1.41,;-.72,.64,;-2.05,1.42,;-3.38,.65,;-3.38,-.89,;-2.06,-1.66,;-2.06,-3.2,;-.72,-3.98,;-3.38,-3.97,;-3.38,-5.51,;-4.71,-3.2,;-6.19,-3.68,;-7.1,-2.43,;-6.19,-1.18,;-4.71,-1.66,;-6.66,-5.15,;-8.17,-5.46,;-9.19,-4.31,;-8.64,-6.92,;-7.61,-8.07,;-6.1,-7.74,;-5.63,-6.28,;-4.12,-5.95,;1.95,.63,;1.94,-.91,;3.28,1.4,;4.62,.63,;5.38,-.71,;6.15,.62,)|
Structure:
Search PDB for entries with ligand similarity: