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Target
Mitogen-activated protein kinase 14
Ligand
BDBM50296657
Substrate
n/a
Meas. Tech.
ChEMBL_582351 (CHEMBL1053415)
IC50
1.1±n/a nM
Citation
Wurz, RP; Pettus, LH; Xu, S; Henkle, B; Sherman, L; Plant, M; Miner, K; McBride, H; Wong, LM; Saris, CJ; Lee, MR; Chmait, S; Mohr, C; Hsieh, F; Tasker, 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
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:
BDBM50296657
Synonyms:
4-chloro-N-cyclopropyl-3-(1-(2,5-difluorophenyl)-7-methyl-6-oxo-6,7-dihydro-1H-pyrazolo[3,4-b]pyridin-4-ylamino)benzamide | CHEMBL560390
Type:
Small organic molecule
Emp. Form.:
C23H18ClF2N5O2
Mol. Mass.:
469.871
SMILES:
Cn1c2n(ncc2c(Nc2cc(ccc2Cl)C(=O)NC2CC2)cc1=O)-c1cc(F)ccc1F