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Information on EC 2.7.11.24 - mitogen-activated protein kinase

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EC Tree
IUBMB Comments
Phosphorylation of specific tyrosine and threonine residues in the activation loop of this enzyme by EC 2.7.12.2, mitogen-activated protein kinase kinase (MAPKK) is necessary for enzyme activation. Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline . A distinguishing feature of all MAPKs is the conserved sequence Thr-Xaa-Tyr (TXY). Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumour necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischaemic injury.
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UNIPROT: Q16539
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Word Map
The enzyme appears in viruses and cellular organisms
Reaction Schemes
+
a [protein]-(L-serine/L-threonine)
=
+
a [protein]-(L-serine/L-threonine) phosphate
Synonyms
mapk, p38, erk1/2, p38 mapk, mitogen-activated protein kinase, map kinase, extracellular signal-regulated kinase, p38 mitogen-activated protein kinase, p38mapk, p38 map kinase, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
MAP kinase
-
mitogen-activated kinase
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p38 MAP kinase
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p38 mitogen activated protein kinase
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p38alpha MAP kinase
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p38alpha mitogen-activated protein kinase
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cp38a
-
-
-
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cp38b
-
-
-
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CSAID binding protein
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-
-
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CSBP
-
-
-
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Cytokine suppressive anti-inflammatory drug binding protein
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-
-
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ERK5
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-
-
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MAP kinase MXI2
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-
-
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MAP kinase p38 beta
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-
-
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MAP kinase p38 delta
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-
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MAP kinase p38 gamma
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-
-
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MAP kinase p38a
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-
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MAP kinase p38alpha
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MAP kinase p38b
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-
-
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MAPK
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-
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mitogen-activated protein kinase
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-
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Mitogen-activated protein kinase p38 beta
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-
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Mitogen-activated protein kinase p38 delta
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-
-
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Mitogen-activated protein kinase p38 gamma
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-
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Mitogen-activated protein kinase p38a
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Mitogen-activated protein kinase p38alpha
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-
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Mitogen-activated protein kinase p38b
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p38b
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-
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SAPK2A
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-
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stress-activated protein kinase 2a
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
phospho group transfer
-
-
-
-
SYSTEMATIC NAME
IUBMB Comments
ATP:protein phosphotransferase (MAPKK-activated)
Phosphorylation of specific tyrosine and threonine residues in the activation loop of this enzyme by EC 2.7.12.2, mitogen-activated protein kinase kinase (MAPKK) is necessary for enzyme activation. Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline [6]. A distinguishing feature of all MAPKs is the conserved sequence Thr-Xaa-Tyr (TXY). Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumour necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischaemic injury.
CAS REGISTRY NUMBER
COMMENTARY hide
142243-02-5
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + ATF2
ADP + a phosphorylated ATF2
show the reaction diagram
substrate in assay, biotinylated ATF2
-
-
?
ATP + MAPKAPK2
ADP + phosphorylated MAPKAPK2
show the reaction diagram
-
-
-
?
additional information
?
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NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + MAPKAPK2
ADP + phosphorylated MAPKAPK2
show the reaction diagram
-
-
-
?
additional information
?
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COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
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(1R,2S)-2-[([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)methyl]cyclohexanol
-
(2R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
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(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
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1-((S)-4-(6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)phthalazin-1-yl)-3-methylpiperazin-1-yl)ethanone
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1-(2,6-dichloro-phenyl)-1-(4-(4-fluorophenyl)thiazol-2-yl)urea
-
1-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol
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1-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol
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2-(4-chlorphenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1,2-dihydropyrazol-3-one
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2-(benzyloxy)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-(ethylsulfanyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)-3-methylbutan-1-ol
-
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)butan-1-ol
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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)ethanol
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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
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2-chloro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-chloro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-fluoro-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
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2-fluoro-4-[2-(phenylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
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2-fluoro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-fluoro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-[(1,5-dimethylhexyl)oxy]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
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2-[4-[3-(4-chlorophenyl)-4-pyrimidin-4-yl-1H-pyrazol-5-yl]piperidin-1-yl]-2-oxoethanol
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3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
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3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
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3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzamide
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3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzonitrile
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3-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
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3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
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3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
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3-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]propan-1-ol
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3-[4-(N-benzyl-N-methylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
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3-[4-(N-benzylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
crystal structure analysis of the inhibitor bound to p38
3-[4-(N-tert-butylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
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3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
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3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
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3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]benzonitrile
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3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
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3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
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3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[4-(4-fluorophenyl)-5-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
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3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
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3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
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3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
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3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
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3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
-
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
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3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-2-yl]methyl]benzonitrile
-
4-(4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl)-N-[(1S)-1-phenylethyl]pyridin-2-amine
-
4-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
-
4-chloro-3-[[1-(2-chlorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-N-cyclopropylbenzamide
-
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(2,5-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-chloro-N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
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4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-chloropyridine
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4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-fluoropyridine
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4-[2-(benzylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-2-fluoropyridine
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4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)pyridin-2-amine
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4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
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4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(2-phenylethyl)pyridin-2-amine
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4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(thiophen-2-ylmethyl)pyridin-2-amine
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4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide
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4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methylbenzoic acid
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4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-N-(2-methoxyethyl)-3-methylbenzamide
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4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
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4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-phenylpyridin-2-amine
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4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
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4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
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4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
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4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(1-phenylethoxy)pyridine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(4-methylphenoxy)pyridine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(tetrahydrofuran-2-ylmethoxy)pyridine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(thiophen-2-ylmethoxy)pyridine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1,2,2-trimethylpropyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-methyl-3-phenylpropyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylpropyl)pyridin-2-amine
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4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-methylbutyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-methylcyclohexyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-phenylpropyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-thiophen-2-ylethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(3-methylbutyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(4-methylcyclohexyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(furan-2-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(naphthalen-1-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-2-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-3-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-4-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydrofuran-2-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(thiophen-2-ylmethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(5-methylfuran-2-yl)methyl]pyridin-2-amine
-
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
4-[[5-(4-fluorophenyl)-4-(2-hydroxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
4-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)-N,N-dimethylphthalazin-1-amine
-
6-chloro-N-cyclopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
-
6-chloro-N-isopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
-
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-1H-indazol-3-amine
-
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isothiazol-3-amine
-
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
-
7-(1-isopropoxyphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
-
7-(1-isopropylphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
-
BIRB 796
a clinical compound, binds to Asp168 and Glu71, and to Met109 in the ATP binding site
Cl-1040
a potent inhibitor of MEK
ethyl 1-[5-([5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]carbamoyl)-2-methylphenyl]-2,3-dihydro-1H-1,2,3-triazole-4-carboxylate
-
N,6-dimethyl-7-(1-((R)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
-
N,6-dimethyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
-
N-(1,2-dimethylpropyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1,2-dimethylpropyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1,2-diphenylethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1,5-dimethylhexyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1-benzothiophen-2-ylmethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1-benzyl-2-phenylethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1-cyclohexylethyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
-
N-(1-methyl-4-phenylbutyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
-
N-(2,3-dihydro-1H-inden-1-yl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(3,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(4-fluorobenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(4-tert-butylbenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-yl)acetamide
-
N-(cyclohexylmethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(furan-2-ylmethyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
-
N-(S)-sec-butyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
-
N-benzyl-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
-
N-benzyl-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-cyclohexyl-4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-cyclohexyl-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-fluorobenzamide
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-5-fluoro-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
N-cyclopropyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
-
N-cyclopropyl-6-methyl-7-(1-o-tolylphthalazin-6-yl)benzo[d]-isoxazol-3-amine
-
N-ethyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
-
N-isopropyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
-
N-[(1R)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[(1S)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[(1S)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[2-(2,5-dimethylphenyl)ethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1R)-1-cyclohexylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1S)-1-cyclohexylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1S)-2-(dimethylamino)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[2-(dimethylamino)-2-methylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[3-(dimethylamino)-2,2-dimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-(N-cyclopropylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(2,2-dimethylpropyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(2-hydroxy-2-methylpropyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(cyclohexylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1-methylpiperidin-3-yl)methyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1-methylpiperidin-4-yl)methyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1R)-1,2,2-trimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1R)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1S)-1,2,2-trimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1S)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-(N-methylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-[N-(pyridin-3-ylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
-
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-[N-(pyridin-4-ylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
-
SB202190
SB203580
SB203580-iodo
-
SB203580-sulfone
-
SB242235
trans-4-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
-
trans-4-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]cyclohexanol
-
[3-amino-2-(1,3-benzodioxol-4-yl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,3-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,4-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,6-dichlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,6-difluoro-4-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,6-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,6-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2,6-dimethylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-chlorophenyl)methanone
-
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-methoxyphenyl)methanone
-
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-trifluoromethylphenyl)methanone
-
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
[3-amino-2-(2-isopropylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
[3-amino-2-(3-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(4-chloro-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
-
[3-amino-2-(4-hydroxy-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-[2-methyl-4-(2-morpholin-4-ylethoxy)phenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
[3-amino-2-[4-(2-methoxyethoxy)-2-methylphenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
MKK3
activation of p38alpha occurs through bisphosphorylation by the dual-specificity Ser/Thr MAP kinases MKK3 and MKK6 on the Thr180-Gly181-Tyr182 motif located on the activation loop
-
MKK6
activation of p38alpha occurs through bisphosphorylation by the dual-specificity Ser/Thr MAP kinases MKK3 and MKK6 on the Thr180-Gly181-Tyr182 motif located on the activation loop
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000008
1-((S)-4-(6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)phthalazin-1-yl)-3-methylpiperazin-1-yl)ethanone
inhibition of p38 MAPK
0.000012
3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.0000016
4-chloro-3-[[1-(2-chlorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-N-cyclopropylbenzamide
-
0.0000033
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.000036
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]benzamide
-
0.0000016
4-chloro-N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000021
4-chloro-N-cyclopropyl-3-[[1-(2,5-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000014
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000017
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.000005
4-chloro-N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000085
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000023
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
0.0000005
6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)-N,N-dimethylphthalazin-1-amine
inhibition of p38 MAPK
0.0000002
6-chloro-N-cyclopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000004
6-chloro-N-isopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.000016
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-1H-indazol-3-amine
inhibition of p38 MAPK
0.000002
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isothiazol-3-amine
inhibition of p38 MAPK
0.0000003
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000004
7-(1-isopropoxyphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000011
7-(1-isopropylphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000003
N,6-dimethyl-7-(1-((R)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000004
N,6-dimethyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000006
N-(6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-yl)acetamide
inhibition of p38 MAPK
0.0000002
N-(S)-sec-butyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
inhibition of p38 MAPK
0.000043
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-fluorobenzamide
-
0.000003
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.00001
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
0.0000027
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.00001
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-5-fluoro-4-methylbenzamide
-
0.0000063
N-cyclopropyl-3-[[1-(2,4-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
0.0000017
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.000003
N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
0.0000046
N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.0000041
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
0.0000077
N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]oxy]-4-methylbenzamide
-
0.0000007
N-cyclopropyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000004
N-cyclopropyl-6-methyl-7-(1-o-tolylphthalazin-6-yl)benzo[d]-isoxazol-3-amine
inhibition of p38 MAPK
0.0000003
N-ethyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
inhibition of p38 MAPK
0.0000005
N-isopropyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
inhibition of p38 MAPK
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000311
(1R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
Homo sapiens
-
0.000235
(1R,2S)-2-[([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)methyl]cyclohexanol
Homo sapiens
-
0.000485
(2R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
Homo sapiens
-
0.000967
(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
Homo sapiens
-
0.0000008
1-((S)-4-(6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)phthalazin-1-yl)-3-methylpiperazin-1-yl)ethanone
Homo sapiens
THP-1 cells
0.000822
1-(2,6-dichloro-phenyl)-1-(4-(4-fluorophenyl)thiazol-2-yl)urea
Homo sapiens
-
0.000146
1-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol
Homo sapiens
-
0.000021
1-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol
Homo sapiens
-
0.000436
2-(benzyloxy)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.000087
2-(ethylsulfanyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.000292
2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
Homo sapiens
-
0.000034
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)-3-methylbutan-1-ol
Homo sapiens
-
0.00001
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)butan-1-ol
Homo sapiens
-
0.000045
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)ethanol
Homo sapiens
-
0.000006
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
Homo sapiens
-
0.001
2-chloro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.00037
2-chloro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.0011
2-fluoro-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.00066
2-fluoro-4-[2-(phenylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.00056
2-fluoro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.00021
2-fluoro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.000641
2-[(1,5-dimethylhexyl)oxy]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.001
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
Homo sapiens
above
0.001
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
Homo sapiens
above
0.000031
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzamide
Homo sapiens
-
0.0000544
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzonitrile
Homo sapiens
-
0.000015
3-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
Homo sapiens
-
0.0000276
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
Homo sapiens
-
0.0000626
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
Homo sapiens
-
0.000061
3-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]propan-1-ol
Homo sapiens
-
0.000029
3-[4-(N-benzyl-N-methylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.00004
3-[4-(N-benzylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000084
3-[4-(N-tert-butylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.001
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
above
0.001
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.000028
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]benzonitrile
Homo sapiens
-
0.000225
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
-
0.00026
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.0000551
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
-
0.00014
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.000191
3-[[4-(4-fluorophenyl)-5-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.000344
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
-
0.000101
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.001
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
above
0.001
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.0000485
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
Homo sapiens
-
0.0000628
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
Homo sapiens
-
0.001
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
above
0.001
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.000078
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
Homo sapiens
-
0.0000954
3-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
Homo sapiens
-
0.001
3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.000148
3-[[5-(4-fluorophenyl)-4-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-2-yl]methyl]benzonitrile
Homo sapiens
-
0.000002
4-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
Homo sapiens
-
0.0029
4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-chloropyridine
Homo sapiens
-
0.00026
4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-fluoropyridine
Homo sapiens
-
0.00195
4-[2-(benzylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-2-fluoropyridine
Homo sapiens
-
0.000248
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)pyridin-2-amine
Homo sapiens
-
0.000199
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
Homo sapiens
-
0.000093
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(2-phenylethyl)pyridin-2-amine
Homo sapiens
-
0.000239
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(thiophen-2-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000042
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide
Homo sapiens
-
0.000491
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methylbenzoic acid
Homo sapiens
-
0.00007
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-N-(2-methoxyethyl)-3-methylbenzamide
Homo sapiens
-
0.000038
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
Homo sapiens
-
0.000051
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-phenylpyridin-2-amine
Homo sapiens
-
0.00004
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
Homo sapiens
-
0.00061
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
Homo sapiens
-
0.00022
4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
Homo sapiens
-
0.00007
4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
Homo sapiens
-
0.00096
4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
Homo sapiens
-
0.000639
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(1-phenylethoxy)pyridine
Homo sapiens
-
0.000033
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(4-methylphenoxy)pyridine
Homo sapiens
-
0.000542
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(tetrahydrofuran-2-ylmethoxy)pyridine
Homo sapiens
-
0.000424
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(thiophen-2-ylmethoxy)pyridine
Homo sapiens
-
0.000023
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1,2,2-trimethylpropyl)pyridin-2-amine
Homo sapiens
-
0.000047
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)pyridin-2-amine
Homo sapiens
-
0.000013
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-methyl-3-phenylpropyl)pyridin-2-amine
Homo sapiens
-
0.00038
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
Homo sapiens
-
0.000068
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylpropyl)pyridin-2-amine
Homo sapiens
-
0.000023
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-methylbutyl)pyridin-2-amine
Homo sapiens
-
0.000013
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-methylcyclohexyl)pyridin-2-amine
Homo sapiens
-
0.000017
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-phenylpropyl)pyridin-2-amine
Homo sapiens
-
0.000023
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(2-thiophen-2-ylethyl)pyridin-2-amine
Homo sapiens
-
0.00009
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(3-methylbutyl)pyridin-2-amine
Homo sapiens
-
0.000015 - 0.000031
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(4-methylcyclohexyl)pyridin-2-amine
0.00006
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(furan-2-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000171
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(naphthalen-1-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.00007
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-2-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000098
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-3-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000119
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(pyridin-4-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.00005
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
Homo sapiens
-
0.000035
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydrofuran-2-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000046
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(thiophen-2-ylmethyl)pyridin-2-amine
Homo sapiens
-
0.000113
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(5-methylfuran-2-yl)methyl]pyridin-2-amine
Homo sapiens
-
0.000916
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
-
0.000859
4-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.0000556
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
-
0.0000871
4-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
-
0.001
4-[[5-(4-fluorophenyl)-4-(2-hydroxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.001
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
above
0.001
4-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
Homo sapiens
above
0.001
4-[[5-(4-fluorophenyl)-4-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
Homo sapiens
above
0.0000004
6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)-N,N-dimethylphthalazin-1-amine
Homo sapiens
THP-1 cells
0.0000013
6-chloro-N-cyclopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000036
6-chloro-N-isopropyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.00012
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-1H-indazol-3-amine
Homo sapiens
THP-1 cells
0.000029
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isothiazol-3-amine
Homo sapiens
THP-1 cells
0.0000036
6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000007
7-(1-isopropoxyphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000011
7-(1-isopropylphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.000018
BIRB 796
Homo sapiens
IC50 with THP-1 cells
0.005
ethyl 1-[5-([5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]carbamoyl)-2-methylphenyl]-2,3-dihydro-1H-1,2,3-triazole-4-carboxylate
Homo sapiens
above, IC50 with THP-1 cells
0.00063
ML3375
Homo sapiens
-
0.00004
ML3403
Homo sapiens
-
0.000001
N,6-dimethyl-7-(1-((R)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000004
N,6-dimethyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.000034
N-(1,2-dimethylpropyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000011
N-(1,2-dimethylpropyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000348
N-(1,2-diphenylethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000026
N-(1,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.00002
N-(1,5-dimethylhexyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000314
N-(1-benzothiophen-2-ylmethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.00215
N-(1-benzyl-2-phenylethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000036
N-(1-cyclohexylethyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000049
N-(1-methyl-4-phenylbutyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000028
N-(2,3-dihydro-1H-inden-1-yl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000126
N-(3,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000173
N-(4-fluorobenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.00134
N-(4-tert-butylbenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0000007
N-(6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)-benzo[d]isoxazol-3-yl)acetamide
Homo sapiens
THP-1 cells
0.00008
N-(cyclohexylmethyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000191
N-(furan-2-ylmethyl)-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0000013
N-(S)-sec-butyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
Homo sapiens
THP-1 cells
0.000282
N-benzyl-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000139
N-benzyl-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000042
N-cyclohexyl-4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.00002
N-cyclohexyl-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0000006
N-cyclopropyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000004
N-cyclopropyl-6-methyl-7-(1-o-tolylphthalazin-6-yl)benzo[d]-isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000004
N-ethyl-6-methyl-7-(1-((S)-3-methylmorpholino)phthalazin-6-yl)benzo[d]isoxazol-3-amine
Homo sapiens
THP-1 cells
0.0000007
N-isopropyl-6-(6-methyl-3-(methylamino)benzo[d]isoxazol-7-yl)phthalazin-1-amine
Homo sapiens
THP-1 cells
0.000153
N-[(1R)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000359
N-[(1S)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000009
N-[(1S)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000082
N-[2-(2,5-dimethylphenyl)ethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.000016
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1R)-1-cyclohexylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000066
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1S)-1-cyclohexylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000035
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[(1S)-2-(dimethylamino)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.00014
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[2-(dimethylamino)-2-methylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000022
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-(4-[N-[3-(dimethylamino)-2,2-dimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.00011
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-(N-cyclopropylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000014
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(2,2-dimethylpropyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000018
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(2-hydroxy-2-methylpropyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000014
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-3-[4-[N-(cyclohexylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]-4-methylbenzamide
Homo sapiens
IC50 with THP-1 cells
0.000028
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1-methylpiperidin-3-yl)methyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.0002
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1-methylpiperidin-4-yl)methyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.00004
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1R)-1,2,2-trimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.000013
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1R)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.000035
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1S)-1,2,2-trimethylpropyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.000027
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-(4-[N-[(1S)-1-phenylethyl]glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl)benzamide
Homo sapiens
IC50 with THP-1 cells
0.00011
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-(N-methylglycyl)-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
Homo sapiens
IC50 with THP-1 cells
0.000038
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-[N-(pyridin-3-ylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
Homo sapiens
IC50 with THP-1 cells
0.000074
N-[5-tert-butyl-2-methoxy-3-[(methylsulfonyl)amino]phenyl]-4-methyl-3-[4-[N-(pyridin-4-ylmethyl)glycyl]-2,3-dihydro-1H-1,2,3-triazol-1-yl]benzamide
Homo sapiens
IC50 with THP-1 cells
0.000026 - 0.0006
SB203580
0.002 - 0.005
SC68376
Homo sapiens
pH 7.2, 25°C
0.001
SKF86002
Homo sapiens
pH 7.2, 25°C
0.00003
trans-4-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
Homo sapiens
-
0.000011
trans-4-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]cyclohexanol
Homo sapiens
-
0.000024
[3-amino-2-(1,3-benzodioxol-4-yl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000037
[3-amino-2-(2,3-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000126
[3-amino-2-(2,4-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000009
[3-amino-2-(2,6-dichlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000005
[3-amino-2-(2,6-difluoro-4-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000017
[3-amino-2-(2,6-difluorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000015
[3-amino-2-(2,6-dimethoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000017
[3-amino-2-(2,6-dimethylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000039
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000024
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-chlorophenyl)methanone
Homo sapiens
-
0.000149
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-methoxyphenyl)methanone
Homo sapiens
-
0.001655
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](2-trifluoromethylphenyl)methanone
Homo sapiens
-
0.000174
[3-amino-2-(2-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
Homo sapiens
-
0.000208
[3-amino-2-(2-isopropylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000023
[3-amino-2-(2-methoxyphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000021
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000411
[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](phenyl)methanone
Homo sapiens
-
0.000228
[3-amino-2-(3-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000038
[3-amino-2-(4-chloro-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000802
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.00253
[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone
Homo sapiens
-
0.000008
[3-amino-2-(4-hydroxy-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.000014
[3-amino-2-[2-methyl-4-(2-morpholin-4-ylethoxy)phenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
0.00002
[3-amino-2-[4-(2-methoxyethoxy)-2-methylphenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone
Homo sapiens
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.2
assay at
7.5
kinase inhibition assay
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
25
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
nonactivated p38 MAP kinase
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
physiological function
additional information
regulation of MAPKs is achieved via a plethora of regulatory proteins including activating MAPKKs and an abundance of deactivating phosphatases. Although all regulatory proteins use an identical interaction site on MAPKs, the common docking and hydrophobic pocket, they use distinct kinase interaction motif (KIM or D-motif) sequences that are present in linear, peptide-like, or well folded protein domains. Fine-tuning necessary to achieve MAPK specificity and regulation among multiple regulatory proteins
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
MK14_HUMAN
360
0
41293
Swiss-Prot
other Location (Reliability: 3)
PDB
SCOP
CATH
UNIPROT
ORGANISM
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D176A/F327S
site-directed mutagenesis of p38alpha, the intrinsically active variant is spontaneously phosphorylated and active toward MK2, the mutant manifests elevated catalytic activity when immunoprecipitated from cells not exposed to any activating signal
additional information
TEMPERATURE STABILITY
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20 - 50
cooperative thermal unfolding profile of p38 MAP kinase, overview
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
His-tagged p38 MAP kinase
recombinant C-terminally His6-tagged p38alpha from Escherichia coli strain BL21 (DE3) RIL by nickel affinity chromatography and gel filtration
recombinant His-tagged isozyme p38alpha MAPK from Escherichia coli by nickel affinity chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expression of His-tagged isozyme p38alpha MAPK in Escherichia coli
recombinant expression of C-terminally His6-tagged p38alpha in Escherichia coli strain BL21 (DE3) RIL
transient expression of wild-type and mutant p38alpha in HEK-293 cells
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
drug development
p38 MAPK inhibitors have significant therapeutic potential for the treatment of rheumatoid arthritis, inflammatory bowel disease, osteoporosis, and many other diseases where aberrant cytokine signaling is the driver of disease
medicine
p38alpha is an attractive target for small molecule drug discovery
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Patel, R.; Lebrun, L.A.; Wang, S.; Howett, L.J.; Thompson, P.A.; Appleman, J.R.; Li, B.
ATLAS - a high-throughput affinity-based screening technology for soluble proteins: technology application using p38 MAP kinase
Assay Drug Dev. Technol.
6
55-68
2008
Homo sapiens (Q16539)
Manually annotated by BRENDA team
Cogan, D.A.; Aungst, R.; Breinlinger, E.C.; Fadra, T.; Goldberg, D.R.; Hao, M.H.; Kroe, R.; Moss, N.; Pargellis, C.; Qian, K.C.; Swinamer, A.D.
Structure-based design and subsequent optimization of 2-tolyl-(1,2,3-triazol-1-yl-4-carboxamide) inhibitors of p38 MAP kinase
Bioorg. Med. Chem. Lett.
18
3251-3255
2008
Homo sapiens (Q16539), Homo sapiens
Manually annotated by BRENDA team
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
Bioorg. Med. Chem. Lett.
18
4006-4010
2008
Homo sapiens (Q16539)
Manually annotated by BRENDA team
Laufer, S.A.; Hauser, D.R.; Domeyer, D.M.; Kinkel, K.; Liedtke, A.J.
Design, synthesis, and biological evaluation of novel tri- and tetrasubstituted imidazoles as highly potent and specific ATP-mimetic inhibitors of p38 MAP kinase: focus on optimized interactions with the enzymes surface-exposed front region
J. Med. Chem.
51
4122-4149
2008
Homo sapiens (Q16539), Homo sapiens
Manually annotated by BRENDA team
Pettus, L.H.; Xu, S.; Cao, G.Q.; Chakrabarti, P.P.; Rzasa, R.M.; Sham, K.; Wurz, R.P.; Zhang, D.; Middleton, S.; Henkle, B.; Plant, M.H.; Saris, C.J.; Sherman, L.; Wong, L.M.; Powers, D.A.; Tudor, Y.; Yu, V.; Lee, M.R.; Syed, R.; Hsieh, F.; Tasker, A.S.
3-amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38alpha mitogen-activated protein kinase
J. Med. Chem.
51
6280-6292
2008
Homo sapiens (Q16539), Homo sapiens
Manually annotated by BRENDA team
Wurz, R.P.; Pettus, L.H.; Henkle, B.; Sherman, L.; Plant, M.; Miner, K.; McBride, H.J.; Wong, L.M.; Saris, C.J.; Lee, M.R.; Chmait, S.; Mohr, C.; Hsieh, F.; Tasker, A.S.
Part 2: 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.
20
1680-1684
2010
Homo sapiens (Q16539), Homo sapiens
Manually annotated by BRENDA team
Lumeras, W.; Caturla, F.; Vidal, L.; Esteve, C.; Balague, C.; Orellana, A.; Dominguez, M.; Roca, R.; Huerta, J.M.; Godessart, N.; Vidal, B.
Design, synthesis, and structure-activity relationships of aminopyridine N-oxides, a novel scaffold for the potent and selective inhibition of p38 mitogen activated protein kinase
J. Med. Chem.
52
5531-5545
2009
Homo sapiens (Q16539), Homo sapiens
Manually annotated by BRENDA team
Kumar, G.; Zettl, H.; Page, R.; Peti, W.
Structural basis for the regulation of the mitogen-activated protein (MAP) kinase p38alpha by the dual specificity phosphatase 16 MAP kinase binding domain in solution
J. Biol. Chem.
288
28347-28356
2013
Homo sapiens (Q16539)
Manually annotated by BRENDA team
Beenstock, J.; Ben-Yehuda, S.; Melamed, D.; Admon, A.; Livnah, O.; Ahn, N.; Engelberg, D.
The p38beta mitogen-activated protein kinase possesses an intrinsic autophosphorylation activity, generated by a short region composed of the alpha-G helix and MAPK insert
J. Biol. Chem.
289
23546-23556
2014
Homo sapiens (Q15759), Homo sapiens (Q16539)
Manually annotated by BRENDA team