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Target
Mitogen-activated protein kinase 14
Ligand
BDBM25992
Substrate
BDBM25978
Meas. Tech.
Fluorescence Polarization Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
140±n/a nM
IC50
870±n/a nM
Citation
 Angell, RM; Angell, TD; Bamborough, P; Brown, D; Brown, M; Buckton, JB; Cockerill, SG; Edwards, CD; Jones, KL; Longstaff, T; Smee, PA; Smith, KJ; Somers, DO; Walker, AL; Willson, M Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR. Bioorg Med Chem Lett 18:324-8 (2008) [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:
BDBM25992
Synonyms:
4-[2-methyl-5-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]-N-{[3-(morpholin-4-ylmethyl)phenyl]methyl}benzamide | benzyl amide analog., 13
Type:
Small organic molecule
Emp. Form.:
C29H30N4O3
Mol. Mass.:
482.5735
SMILES:
Cc1nnc(o1)-c1ccc(C)c(c1)-c1ccc(cc1)C(=O)NCc1cccc(CN2CCOCC2)c1
Structure:
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Substrate
Name:
BDBM25978
Synonyms:
2-(6-amino-3-imino-3H-xanthen-9-yl)-5-[({4-[4-(4-chloro-3-hydroxyphenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl]phenyl}methyl)carbamoyl]benzoic acid | 2-(6-amino-3-imino-3H-xanthen-9-yl)-5-{[({4-[4-(4-chloro-3-hydroxyphenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenyl}methyl)amino]carbonyl}benzoic acid | Rhodamine-green Labelled Fluoroligand
Type:
fluorescent ligand
Emp. Form.:
C42H29ClN6O5
Mol. Mass.:
733.17
SMILES:
Nc1ccc2c(-c3ccc(cc3C(O)=O)C(=O)NCc3ccc(cc3)-c3nc(c([nH]3)-c3ccc(Cl)c(O)c3)-c3ccncc3)c3ccc(=N)cc3oc2c1 |(20.56,-12.19,;21.37,-13.5,;22.91,-13.48,;23.71,-14.78,;23.1,-16.17,;24.02,-17.42,;25.58,-17.36,;26.31,-18.73,;27.83,-18.86,;28.72,-17.6,;28,-16.29,;26.45,-16.1,;26.39,-14.56,;25.44,-13.37,;27.85,-13.92,;30.26,-17.52,;30.99,-16.16,;31.06,-18.84,;30.24,-20.16,;30.99,-21.5,;32.53,-21.48,;33.3,-22.81,;32.51,-24.14,;30.97,-24.15,;30.2,-22.82,;33.27,-25.45,;32.66,-26.91,;33.83,-27.98,;35.18,-27.19,;34.83,-25.64,;36.6,-27.75,;36.82,-29.27,;38.21,-29.9,;39.45,-29,;40.87,-29.61,;39.25,-27.47,;40.49,-26.54,;37.84,-26.84,;33.62,-29.48,;34.82,-30.44,;34.66,-31.96,;33.25,-32.57,;32.02,-31.63,;32.2,-30.1,;23.27,-18.79,;24.02,-20.13,;23.26,-21.47,;21.72,-21.48,;20.95,-22.81,;20.95,-20.14,;21.72,-18.8,;20.85,-17.53,;21.55,-16.16,;20.7,-14.88,)|
Structure:
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