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Target
Mitogen-activated protein kinase 14
Ligand
BDBM15745
Substrate
myelin basic protein
Meas. Tech.
In Vitro Kinase Assay
IC50
340±n/a nM
Citation
Goldstein, DM; Alfredson, T; Bertrand, J; Browner, MF; Clifford, K; Dalrymple, SA; Dunn, J; Freire-Moar, J; Harris, S; Labadie, SS; La Fargue, J; Lapierre, JM; Larrabee, S; Li, F; Papp, E; McWeeney, D; Ramesha, C; Roberts, R; Rotstein, D; San Pablo, B; Sjogren, EB; So, OY; Talamas, FX; Tao, W; Trejo, A; Villasenor, A; Welch, M; Welch, T; Weller, P; Whiteley, PE; Young, K; Zipfel, S Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase. J Med Chem 49:1562-75 (2006) [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:
BDBM15745
Synonyms:
1-(2,4-difluorophenyl)-4-{[3-(pyridin-3-yloxy)phenyl]carbonyl}-1H-pyrazol-5-amine | [5-Amino-1-(2,4-difluorophenyl)-1H-pyrazol-4-yl]-[3-(1-oxypyridin-3-yl)phenyl]methanone | aminopyrazole 56
Type:
Small organic molecule
Emp. Form.:
C21H14F2N4O2
Mol. Mass.:
392.3583
SMILES:
Nc1c(cnn1-c1ccc(F)cc1F)C(=O)c1cccc(Oc2cccnc2)c1
Substrate
Name:
myelin basic protein
Synonyms:
MBP | MBP_HUMAN | Myelin A1 protein | Myelin membrane encephalitogenic protein | biotin-MBP protein | biotin-myelin basic protein
Type:
Other Protein Type
Mol. Mass.:
33133.33
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
304
Sequence:
MGNHAGKRELNAEKASTNSETNRGESEKKRNLGELSRTTSEDNEVFGEADANQNNGTSSQDTAVTDSKRTADPKNAWQDAHPADPGSRPHLIRLFSRDAPGREDNTFKDRPSESDELQTIQEDSAATSESLDVMASQKRPSQRHGSKYLATASTMDHARHGFLPRHRDTGILDSIGRFFGGDRGAPKRGSGKDSHHPARTAHYGSLPQKSHGRTQDENPVVHFFKNIVTPRTPPPSQGKGRGLSLSRFSWGAEGQRPGFGYGGRASDYKSAHKGFKGVDAQGTLSKIFKLGGRDSRSGSPMARR