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Literature summary for 2.7.11.24 extracted from

  • Kim, D.K.; Lim, J.H.; Lee, J.A.; Dewang, P.M.
    Synthesis and biological evaluation of trisubstituted imidazole derivatives as inhibitors of p38alpha mitogen-activated protein kinase (2008), Bioorg. Med. Chem. Lett., 18, 4006-4010.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of His-tagged isozyme p38alpha MAPK in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(2,6-dichloro-phenyl)-1-(4-(4-fluorophenyl)thiazol-2-yl)urea
-
Homo sapiens
2-[4-[3-(4-chlorophenyl)-4-pyrimidin-4-yl-1H-pyrazol-5-yl]piperidin-1-yl]-2-oxoethanol
-
Homo sapiens
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
-
Homo sapiens
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
-
Homo sapiens
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzamide
-
Homo sapiens
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzonitrile
-
Homo sapiens
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
-
Homo sapiens
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
-
Homo sapiens
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]benzonitrile
-
Homo sapiens
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[4-(4-fluorophenyl)-5-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-2-yl]methyl]benzonitrile
-
Homo sapiens
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
4-[[5-(4-fluorophenyl)-4-(2-hydroxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
Homo sapiens
4-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
Homo sapiens
BIRB-796
-
Homo sapiens
SB242235
-
Homo sapiens
SCIO-469
-
Homo sapiens
TAK-715
-
Homo sapiens
VX-702
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q16539 isozyme p38alpha MAPK
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged isozyme p38alpha MAPK from Escherichia coli by nickel affinity chromatography Homo sapiens

Synonyms

Synonyms Comment Organism
p38alpha mitogen-activated protein kinase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000276
-
-
Homo sapiens 3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
0.000028
-
-
Homo sapiens 3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]benzonitrile
0.000031
-
-
Homo sapiens 3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzamide
0.0000485
-
-
Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
0.0000544
-
-
Homo sapiens 3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzonitrile
0.0000551
-
-
Homo sapiens 3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.0000556
-
-
Homo sapiens 4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.0000626
-
-
Homo sapiens 3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
0.0000628
-
-
Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
0.000078
-
-
Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
0.0000871
-
-
Homo sapiens 4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.0000954
-
-
Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
0.000101
-
-
Homo sapiens 3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
0.00014
-
-
Homo sapiens 3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.000148
-
-
Homo sapiens 3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-2-yl]methyl]benzonitrile
0.000191
-
-
Homo sapiens 3-[[4-(4-fluorophenyl)-5-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
0.000225
-
-
Homo sapiens 3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.00026
-
-
Homo sapiens 3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.000344
-
-
Homo sapiens 3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
0.000822
-
-
Homo sapiens 1-(2,6-dichloro-phenyl)-1-(4-(4-fluorophenyl)thiazol-2-yl)urea
0.000859
-
-
Homo sapiens 4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.000916
-
-
Homo sapiens 4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.001
-
above Homo sapiens 3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
0.001
-
above Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 4-[[5-(4-fluorophenyl)-4-(2-hydroxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
0.001
-
above Homo sapiens 3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
0.001
-
above Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.001
-
above Homo sapiens 3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
0.001
-
above Homo sapiens 3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.001
-
above Homo sapiens 4-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
0.001
-
above Homo sapiens 4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide