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Information on EC 2.7.11.24 - mitogen-activated protein kinase and Organism(s) Homo sapiens and UniProt Accession P27361

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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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Homo sapiens
UNIPROT: P27361
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Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected 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
extracellular regulated kinase
-
extracellular signal-regulated kinase
-
extracellular signal-regulated kinase 1
-
mitogen-activated protein kinase 3
-
mitogen-activated protein kinase p44erk1
-
c-Jun N-terminal kinase
c-jun N-terminal kinase 1
c-Jun N-terminal kinase 2
c-Jun N-terminal kinase 3
c-Jun NH2-terminal kinase
-
-
c-jun NH2-terminal MAPK
-
-
cp38a
-
-
-
-
cp38b
-
-
-
-
CSAID binding protein
-
-
-
-
CSBP
-
-
-
-
Cytokine suppressive anti-inflammatory drug binding protein
-
-
-
-
ERK5
-
-
-
-
extracellular regulated kinase
-
extracellular signal-regulated kinase
-
extracellular signal-regulated kinase 1/2
-
-
extracellular signal-regulated kinase 2
extracellular signal-regulated kinases-1/2
-
-
extracellular signal-related kinase
-
-
JNK/SAPK1c
-
-
JNK1/2
-
-
JNK1alpha1
-
JNK2alpha2
-
MAP kinase
MAP kinase MXI2
-
-
-
-
MAP kinase p38 beta
-
-
-
-
MAP kinase p38 delta
-
-
-
-
MAP kinase p38 gamma
-
-
-
-
MAP kinase p38a
-
-
-
-
MAP kinase p38alpha
-
-
-
-
MAP kinase p38b
-
-
-
-
MAPK kinase
-
-
mitogen-activated kinase
mitogen-activated protein kinase
mitogen-activated protein kinase 1
-
mitogen-activated protein kinase 10
-
mitogen-activated protein kinase 11
-
mitogen-activated protein kinase 13
-
mitogen-activated protein kinase 4
-
mitogen-activated protein kinase 6
-
mitogen-activated protein kinase 7
-
mitogen-activated protein kinase 8
-
mitogen-activated protein kinase 9
-
Mitogen-activated protein kinase p38 beta
-
-
-
-
Mitogen-activated protein kinase p38 delta
-
-
-
-
Mitogen-activated protein kinase p38 gamma
-
-
-
-
Mitogen-activated protein kinase p38a
-
-
-
-
Mitogen-activated protein kinase p38alpha
-
-
-
-
Mitogen-activated protein kinase p38b
-
-
-
-
mitogen-activated protein kinase/extracellular signal-regulated kinase 1/2 kinase
-
-
p38 MAP kinase
p38 MAPK
p38 MAPKalpha
-
-
p38 mitogen activated protein kinase
-
p38 mitogen-activated protein kinase
p38 mitogen-activated protein kinase alpha
-
-
p38 protein
-
-
p38-delta mitogen-activated protein kinase
-
p38-MAPK
-
-
p38alpha
p38alpha MAP kinase
p38alpha mitogen-activated protein kinase
P38alpha-MAPKAP kinase 2
-
-
p38b
-
-
-
-
p38beta
p38delta
p38gamma
p38MAPK
-
-
p493F12 kinase
-
SAPK
-
-
SAPK2A
-
-
-
-
SAPK2a/p38
-
-
SAPK2b/p38beta
-
-
SAPK3/p38gamma
-
-
SAPK4/p38delta
-
-
SAPKalphaI/JNK2
-
-
signal-regulated kinase 3
-
stress-activated protein kinase 2a
-
-
-
-
stress-activated protein kinase-4
-
additional information
-
the enzyme belongs to the MAPK superfamily of enzymes
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
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 + focal adhesion kinase
ADP + phosphorylated focal adhesion kinase
show the reaction diagram
phosphorylation of FAK at S910, which promotes the disassembly of focal adhesion (hemidesmosome disruption) during cell migration
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
autophosphorylation
-
-
?
ATP + a protein
ADP + a phosphoprotein
show the reaction diagram
ATP + ATF-2
ADP + phosphorylated ATF-2
show the reaction diagram
ATP + ATF2
ADP + a phosphorylated ATF2
show the reaction diagram
substrate in assay, biotinylated ATF2
-
-
?
ATP + ATF2
ADP + phosphorylated ATF2
show the reaction diagram
ATP + Bcl-2
ADP + phosphorylated Bcl-2
show the reaction diagram
-
-
-
?
ATP + c-Jun
ADP + phosphorylated c-Jun
show the reaction diagram
ATP + c-Jun activation domain
ADP + phosphorylated c-Jun activation domain
show the reaction diagram
ATP + c-Jun transcription factor
ADP + phosphorylated c-Jun transcription factor
show the reaction diagram
-
JNK phosphorylates the N-terminal transactivation domain of c-Jun transcription factor
-
-
?
ATP + Elk-1
ADP + phosphorylated Elk-1
show the reaction diagram
ATP + FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2
ADP + phosphorylated FITC-Aca-Ala-Ala-Ala-Thr-Gly-Pro-Leu-Ser-Pro-Gly-Pro-Phe-Ala-NH2
show the reaction diagram
-
FITC-labeled ERK substrate peptide
-
-
?
ATP + focal adhesion kinase
ADP + phosphorylated focal adhesion kinase
show the reaction diagram
phosphorylation of FAK at S910, which promotes the disassembly of focal adhesion (hemidesmosome disruption) during cell migration
-
-
?
ATP + GST-c-Jun
ADP + phosphorylated GST-c-Jun
show the reaction diagram
-
substrate in kinase activity assay
-
-
?
ATP + heat shock factor 1
ADP + phosphorylated heat shock factor 1
show the reaction diagram
-
phosphorylation at Ser-326, Ser-303 and Ser-307, better substrate for p38gamma than for any of the other p38 isoforms
-
-
?
ATP + human glucocorticoid receptor
ADP + phosphorylated human glucocorticoid receptor
show the reaction diagram
ATP + IRS-1
ADP + phosphorylated IRS-1
show the reaction diagram
-
phosphorylation of the insulin receptor substrate IRS-1 at serine 307
-
-
?
ATP + Lin-1
ADP + phosphorylated Lin-1
show the reaction diagram
ATP + MAPK
ADP + phosphorylated MAPK
show the reaction diagram
-
-
-
-
?
ATP + MAPKAP kinase-2
ADP + phosphorylated MAPKAP kinase-2
show the reaction diagram
-
-
-
?
ATP + MAPKAP kinase-3
ADP + phosphorylated MAPKAP kinase-3
show the reaction diagram
-
-
-
?
ATP + MAPKAPK2
ADP + phosphorylated MAPKAPK2
show the reaction diagram
-
-
-
?
ATP + MAPKAPK2-peptide
ADP + phosphorylated MAPKAPK2-peptide
show the reaction diagram
-
the peptide substrate is derived from a sequence of a mitogen-activated protein kinase activated protein kinase-2, MAPKAPK2, phopshorylation site
-
-
?
ATP + MK2
ADP + phosphorylated MK2
show the reaction diagram
-
-
-
-
?
ATP + MMP-9
ADP + phosphorylated MMP-9
show the reaction diagram
ATP + multifunctional protein CAD
ADP + phosphorylated multifunctional protein CAD
show the reaction diagram
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
show the reaction diagram
-
substrate in in vitro kinase assay
-
-
?
ATP + Net
ADP + phosphorylated Net
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
autophosphorylates both Thr and Tyr residues
-
-
?
ATP + protein APP
ADP + phosphorylated protein APP
show the reaction diagram
-
-
-
?
ATP + protein ATF2
ADP + phosphorylated protein ATF2
show the reaction diagram
ATP + protein EGFRP
ADP + phosphorylated protein EGFRP
show the reaction diagram
-
epidermal growth factor receptor peptide, substrate in kinase activity assay
-
-
?
ATP + transcription factor ATF2
ADP + phosphorylated transcription factor ATF2
show the reaction diagram
-
-
-
?
ATP + transcription factor Elk-1
ADP + phosphorylated transcription factor Elk-1
show the reaction diagram
-
-
-
?
ATP + transcription factor SAP-1
ADP + phosphorylated transcription factor SAP-1
show the reaction diagram
-
-
-
?
additional information
?
-
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 + ATF2
ADP + phosphorylated ATF2
show the reaction diagram
-
-
-
?
ATP + c-Jun
ADP + phosphorylated c-Jun
show the reaction diagram
ATP + Elk-1
ADP + phosphorylated Elk-1
show the reaction diagram
an ETS family transcription factor
-
-
?
ATP + human glucocorticoid receptor
ADP + phosphorylated human glucocorticoid receptor
show the reaction diagram
-
specific phosphorylation at Ser211 by p38 MAPK, p38 MAPK is a mediator in glucocorticoid-induced apoptosis of lymphoid cells, interaction of MAPK and glucocorticoid pathways, overview
-
-
?
ATP + Lin-1
ADP + phosphorylated Lin-1
show the reaction diagram
substrate of ERK2, negative regulation of Lin-1
-
-
?
ATP + MAPKAPK2
ADP + phosphorylated MAPKAPK2
show the reaction diagram
-
-
-
?
ATP + MMP-9
ADP + phosphorylated MMP-9
show the reaction diagram
-
activity of p38 MAP kinase, TNF-alpha stimulates MMP-9 expression via the p38 MAP kinase signaling pathway in 5637 cells, and p38 MAP kinase-mediated MMP-9 gene regulation in response to TNF-alpha is involved in the NF-kappaB response element in 5637 cells, regulation, overview
-
-
?
ATP + multifunctional protein CAD
ADP + phosphorylated multifunctional protein CAD
show the reaction diagram
-
CAD initiates and regulates de novo pyrimidine biosynthesis and is activated by phosphorylation at Thr456 by nuclear MAPKs, nuclear import of CAD is required for optimal cell growth
-
-
?
ATP + Net
ADP + phosphorylated Net
show the reaction diagram
an ETS family transcription factor
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
partially restores the ability of the protein to dimerize
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
PD98059
an ERK inhibitor
U0126
(1R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
-
(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
-
(2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide
-
RO4927350
(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
-
(3R)-3-([4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)butanoic acid
-
-
(R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide
(R)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-hydroxyphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(2-trifluoromethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(3-fluoro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(4-chloro-2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(4-chloro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-4-[2-(benzo[d]1,3-dioxolylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
(S)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,2-difluorobenzo[d][1,3]dioxol-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydro-1H-inden-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydrobenzo[b][1,4]dioxin-5-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2(5,6,7,8-tetrahydronaphthalen-1-ylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
(S)-N-[1-(3-methylphenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
1-((S)-4-(6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)phthalazin-1-yl)-3-methylpiperazin-1-yl)ethanone
-
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
-
1-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol
-
1-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
2,2'-disulfanediylbis(1,3-benzothiazole)
-
-
2-(3-tert-butyl-1-methyl-1H-pyrazol-5-yl)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide
-
-
2-(4-chlorphenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1,2-dihydropyrazol-3-one
-
2-(5-tert-butyl-2-methylfuran-3-yl)-2-oxo-N-[4-(pyrimidin-2-ylamino)-5,8-dihydronaphthalen-1-yl]acetamide
-
-
2-(5-tert-butyl-2-methylfuran-3-yl)-2-oxo-N-[4-(pyrimidin-4-ylamino)-5,8-dihydronaphthalen-1-yl]acetamide
-
-
2-(5-tert-butyl-2-methylfuran-3-yl)-N-(4-[[6-(morpholin-4-ylmethyl)pyridin-3-yl]methyl]-5,8-dihydronaphthalen-1-yl)-2-oxoacetamide
-
-
2-(5-tert-butyl-2-methylfuran-3-yl)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide
-
-
2-(benzyloxy)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-(ethylamino)-N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
2-(ethylsulfanyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
-
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
-
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)ethanol
-
2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
-
2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
-
2-bromothiazole-5-carboxylic acid
-
inhibition of p38alpha MAP kinase
2-chloro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-chloro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-fluoro-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
-
2-fluoro-4-[2-(phenylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine
-
2-fluoro-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-fluoro-4-[4-(4-fluorophenyl)-2-(phenylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-[(1,5-dimethylhexyl)oxy]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
-
2-[(1-methylethyl)amino]-N-[2-methyl-5-(1H-pyrazol-5-ylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
2-[(1-methylethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
2-[(1-methylethyl)amino]-N-[2-methyl-5-[(1-methyl-1H-pyrazol-5-yl)carbamoyl]phenyl]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
2-[(2,4-dinitrophenyl)sulfanyl]-1,3-benzoxazole
-
-
2-[(2-methoxyethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
-
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
-
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole-5-sulfonic acid
-
-
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-5-(trifluoromethyl)-1H-benzimidazole
-
-
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl][1,3]thiazolo[4,5-b]pyridine
-
-
2-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]-2-(hydroxyamino)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]acetamide
-
-
2-[4-[3-(4-chlorophenyl)-4-pyrimidin-4-yl-1H-pyrazol-5-yl]piperidin-1-yl]-2-oxoethanol
-
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
-
PH-797804, ATP-competitive, readily reversible inhibitor of the alpha isoform of human p38 MAP kinase
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
-
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
-
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzamide
-
3-([4-[2-(cyclopropylamino)pyrimidin-4-yl]-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl)benzonitrile
-
3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
-
3-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol
-
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzamide
-
3-([5-[2-(cyclopropylamino)pyrimidin-4-yl]-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl)benzonitrile
-
3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
-
3-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]propan-1-ol
-
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N,4-dimethylbenzamide
-
inhibition of p38alpha MAP kinase
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N-ethyl-4-methylbenzamide
-
inhibition of p38alpha MAP kinase
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
-
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
-
3-[[1-(2,4-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]-4-methylbenzamide
-
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[4-(2-aminopyrimidin-4-yl)-5-(4-fluorophenyl)-1H-imidazol-2-yl]methyl]benzonitrile
-
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[4-(4-fluorophenyl)-5-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[4-(4-fluorophenyl)-5-(2-[[(1S)-1-phenylethyl]amino]pyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[4-(4-fluorophenyl)-5-[2-[(4-methoxybenzyl)amino]pyrimidin-4-yl]-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[5-(2-aminopyrimidin-4-yl)-4-(4-fluorophenyl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzamide
-
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-1-yl]methyl]benzonitrile
-
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzamide
-
3-[[5-(4-fluorophenyl)-4-(2-methoxypyrimidin-4-yl)-1H-imidazol-2-yl]methyl]benzonitrile
-
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
-
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-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3,4-thiadiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol
-
-
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-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
-
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
-
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(2,6-difluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(3-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-chloro-N-cyclopropyl-3-[[1-(4-fluorophenyl)-7-methyl-1H-pyrazolo[3,4-d]pyridazin-4-yl]amino]benzamide
-
4-[(1H-benzimidazol-2-ylsulfanyl)methyl]benzoic acid
-
-
4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-chloropyridine
-
4-[2-(benzylsulfanyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-fluoropyridine
-
4-[2-(benzylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-2-fluoropyridine
-
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)pyridin-2-amine
-
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
-
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(2-phenylethyl)pyridin-2-amine
-
4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]-N-(thiophen-2-ylmethyl)pyridin-2-amine
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
-
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylpiperidin-4-yl)pyrimidin-2-amine
-
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
-
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
-
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-2-amine
-
-
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-methylpyrimidin-2-amine
-
-
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methyl-N-(2-morpholin-4-ylethyl)benzamide
-
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-3-methylbenzoic acid
-
4-[3-amino-4-(2,4-difluorobenzoyl)-1-oxidopyridin-2-yl]-N-(2-methoxyethyl)-3-methylbenzamide
-
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(tetrahydro-2H-pyran-4-yl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-phenylpyridin-2-amine
-
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
-
4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1S)-1-phenylethyl]pyridin-2-amine
-
4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-(1-phenylethyl)pyridin-2-amine
-
4-[4-(4-fluorophenyl)-1-methyl-2-(methylsulfanyl)-1H-imidazol-5-yl]-N-[(1R)-1-phenylethyl]pyridin-2-amine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(1-phenylethoxy)pyridine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(4-methylphenoxy)pyridine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(tetrahydrofuran-2-ylmethoxy)pyridine
-
4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]-2-(thiophen-2-ylmethoxy)pyridine
-
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
-
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-[[(6-amino-9H-purin-8-yl)sulfanyl]methyl]benzoic acid
-
-
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
-
5,6-dichloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
5-(5-nitrothiazol-2-ylthio)-N-((tetrahydrofuran-2-yl)methyl)-1,3,4-thiadiazol-2-amine
-
-
5-(5-nitrothiazol-2-ylthio)-N-propyl-1,3,4-thiadiazol-2-amine
-
-
5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
-
5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
-
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
-
5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
-
5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
-
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
-
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
-
5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
-
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
-
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
5-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
5-nitro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
-
-
5-tert-butyl-N-cyclopropyl-2-methoxy-3-[2-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-2-oxo-acetylamino]-benzamide
-
KR-003048
6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)-N,N-dimethylphthalazin-1-amine
-
6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
-
6-chloro-2-[(4-methyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]-1,3-benzothiazole
-
-
6-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
-
6-chloro-2-[[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
-
6-chloro-2-[[5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
-
6-chloro-2-[[5-(2-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
-
-
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-ethoxy-1,3-benzothiazole-2-sulfonamide
-
-
6-ethoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
-
-
6-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
-
-
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
-
6-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-2-amine
-
-
6-[5-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl]quinoline
-
-
7-(1-isopropoxyphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
-
7-(1-isopropylphthalazin-6-yl)-N,6-dimethylbenzo[d]isoxazol-3-amine
-
7-(6-N-phenylaminohexyl)amino-2H-anthra[1,9-cd]pyrazol-6-one
AV-7
8-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-6-amine
-
-
adalimumab
-
-
-
alsterpaullone
-
inhibition of JNK/SAPK1c, SAPK2a/p38, SAPK2b/p38beta, SAPK3/p38gamma, and SAPK4/p38delta
AZD6244
-
ARRY-142886, MEK1/2 inhibitor
BIRB 796
BIRB-796
BIRB0796
-
-
-
BIRB796
-
-
C2-alkylaminothiazole
-
-
calcium diphosphate
-
crystals in plasma inhibit the p38 MAP kinase mediating the activation of neutrophils and repression of TNF-alpha-induced apoptosis
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
-
FR180204
-
ERK inhibitor, 5-(2-phenyl-pyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-ylamine
furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide
inhibits JNK2alpha2 enzyme in vitro
indirubin-3'-monoxime
-
79% inhibition at 0.01 mM of JNK/SAPK1c, 17% inhibition at 0.01 mM of SAPK2a/p38, 55% inhibition at 0.01 mM of SAPK2b/p38beta, 26% inhibition at 0.01 mM of SAPK3/p38gamma, and 35% inhibition at 0.01 mM of SAPK4/p38delta
kenpaullone
-
slight inhibition of SAPK2a/p38 and SAPK3/p38gamma, no inhibition of SAPK4/p38delta, JNK/SAPK1c, SAPK2b/p38beta, and SAPK4/p38delta
MKK4
-
MKK4 mutant F48K
the D-site from enzyme MKK4 competitively inhibits JNK-mediated phosphorylation of c-Jun and ATF2, but to a lesser degree compared to the wild-type MKK4
-
MKK4 mutant L44I
-
Mycophenolic acid
-
-
N,4-dimethyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
-
inhibition of p38alpha MAP kinase
N,4-dimethyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
-
inhibition of p38alpha MAP kinase
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-(1-methylethyl)-4-(1H-pyrazol-4-yl)pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-(3-piperidin-3-yl-1H-pyrazol-4-yl)pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
N-(2,3-dihydro-1H-inden-1-yl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(2-chloro-6-methylphenyl)-2-(cyclobutylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(2-chloro-6-methylphenyl)-2-(ethylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(2-chloro-6-methylphenyl)-2-(phenylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(2-chloro-6-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(2-chloro-6-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(2-methoxyethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
-
N-(3,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(3,4-dimethoxyphenethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
-
N-(4-fluorobenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(4-methoxybenzyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
-
N-(4-tert-butylbenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-(5-carbamoyl-2-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-(5-carbamoyl-2-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
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-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-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-4-methyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
-
inhibition of p38alpha MAP kinase
N-ethyl-4-methyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
-
inhibition of p38alpha MAP kinase
N-ethyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-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-sec-butyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
-
-
N-[(1R)-1-cyclohexylethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[(1S)-1-(3-chloro-4-fluorophenyl)-2-hydroxyethyl]-4-[4-(3-chlorophenyl)-1H-pyrazol-3-yl]-1H-pyrrole-3-carboxamide
-
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-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
-
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
-
N-[2-(2,5-dimethylphenyl)ethyl]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
-
N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
-
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-[[(1S)-1-methylpropyl]amino]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
-
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
-
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-2-(propylamino)-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
N-[5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
-
inhibition of p38alpha MAP kinase
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
-
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
-
-
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
-
-
panduratin A
-
-
PD098059
-
selective inhibitor of mitogen-activated extracellular regulated kinase phosphorylation, arrests cells in G(0)/G(1), increases P21/waf1 antigen expression
PD98059
pep-JIP1
-
peptide corresponding to the D-domain of JIP-1, final sequence of the most extensively used peptide is GRKKRRQRRRPPRPKRPTTLNLFPQVPRSQDT
purvalanol
-
16% inhibition at 0.01 mM of JNK/SAPK1c, no inhibition of SAPK2a/p38, SAPK3/p38gamma, and SAPK4/p38delta
S-1,3-benzothiazol-2-yl (2Z)-(2-amino-1,3-thiazol-4-yl)(methoxyimino)ethanethioate
-
-
SB 203580
-
no preference for either active or inactive p38alpha, no preincubation required to achieve maximum inhibition
SB202
-
p38 inhibitor SB202
SB202190
SB203580
SB203580-iodo
-
SB203580-sulfone
-
SB242235
SP600125
SR3451
-
-
SR3576
-
-
SR3582
-
-
SR3583
-
-
SR4018
-
-
SR4276
-
-
SR4326
-
-
SR4642
-
-
SR4643
-
-
tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
-
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
-
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
-
U0126
[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
-
[Nle4, D-Phe7]alpha-melanocyte stimulating hormone
-
NDP-MSH, the melanocortin agonist dose-dependently inhibits JNK activity in HEK-293 cells stably expressing the human melanocortin receptor type 4
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
mycosporine-glycine
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
porphyra
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
shinorine
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
amitriptyline
-
up-regulates ERK1/2 phosphorylation and activity 8fold at 0.01 mM, the addition of nor-binaltorphimine (100 nM) reduces the amitriptyline stimulatory effect by 70%
citrinin
-
the exposure of HEK-293 and HeLa cells to citrinin results in a dose-dependent increase in the phosphorylation of ERK1/2 and JNK
cytokines
-
glucocorticoids
-
activate p38 MAPK, e.g. by induction of activating MKK3
-
interleukin-1beta
-
activates the MAPKs, dexamethasone inhibits this activation
-
interleukin-I
-
-
-
lipopolysaccharide
-
-
mitogen-activated protein kinase kinase 6
-
MKK6
-
MKK3
-
MKK6
-
mycosporine-glycine
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
phenethyl isothiocyanate
-
the enzyme is activated by exposure to 0.02 mM phenethyl isothiocyanate
porphyra
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
Porphyromonas gingivalis supernatant
-
-
-
purvalanol
-
17% activation of SAPK2b/p38beta
Ras
Ras induces phosphorylation of c-Jun by JNKs
-
shinorine
mycosporine-like amino acids shinorine, mycosporine-glycine, and porphyra are purified from Chlamydomonas hedlyei and Porphyra yezoensis activate kinase ERK and JNK, especially JNK
temozolomide
-
-
thapsigargin
-
stimulates 4-5fold the expression of p44/p42
TNF-alpha
-
transforming growth factor-beta
-
i.e. TGF-beta, activates p38, butenoside inhibits this activation
-
tumor necrosis factor-alpha
-
-
-
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0019
protein ATF2
-
pH 7.6, 27°C, purified, recombinant detagged, activated p38 MAPKalpha
-
additional information
additional information
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.98
protein ATF2
-
pH 7.6, 27°C, purified, recombinant detagged, activated p38 MAPKalpha
-
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000315
(3R)-3-([4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)butanoic acid
-
-
0.00067
(R)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
0.000002 - 0.000003
(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
0.000002
(S)-4-[2-(2-chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl]- N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM, potent, selective, and orally bioavailable inhibitor of ERK
0.000002
(S)-4-[2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000003
(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000002
(S)-4-[2-(2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000004
(S)-4-[2-(2-hydroxyphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000002
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000004
(S)-4-[2-(2-trifluoromethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000034
(S)-4-[2-(3-fluoro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000005
(S)-4-[2-(4-chloro-2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000005
(S)-4-[2-(4-chloro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
-
0.000002
(S)-4-[2-(benzo[d]1,3-dioxolylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,2-difluorobenzo[d][1,3]dioxol-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydro-1H-inden-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000015
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydrobenzo[b][1,4]dioxin-5-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
0.000013
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2(5,6,7,8-tetrahydronaphthalen-1-ylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
-
0.000002
(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-N-[1-(3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
0.000002
(S)-N-[1-(3-methylphenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide
Ki below 0.000002 mM
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
0.00007
2-(3-tert-butyl-1-methyl-1H-pyrazol-5-yl)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide
-
-
0.00046
2-(5-tert-butyl-2-methylfuran-3-yl)-2-oxo-N-[4-(pyrimidin-2-ylamino)-5,8-dihydronaphthalen-1-yl]acetamide
-
-
0.000059
2-(5-tert-butyl-2-methylfuran-3-yl)-2-oxo-N-[4-(pyrimidin-4-ylamino)-5,8-dihydronaphthalen-1-yl]acetamide
-
-
0.00004
2-(5-tert-butyl-2-methylfuran-3-yl)-N-(4-[[6-(morpholin-4-ylmethyl)pyridin-3-yl]methyl]-5,8-dihydronaphthalen-1-yl)-2-oxoacetamide
-
-
0.000041
2-(5-tert-butyl-2-methylfuran-3-yl)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]-2-oxoacetamide
-
-
0.000049
2-[3-tert-butyl-1-(3-methylphenyl)-1H-pyrazol-5-yl]-2-(hydroxyamino)-N-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]acetamide
-
-
0.0000058
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
-
-
0.000036
3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
-
-
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
-
0.000048
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
-
-
0.00157
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylpiperidin-4-yl)pyrimidin-2-amine
-
-
0.000027
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
-
-
0.000026
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
-
-
0.000151
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-2-amine
-
-
0.00206
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-methylpyrimidin-2-amine
-
-
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
0.00273
N-(1-methylethyl)-4-(1H-pyrazol-4-yl)pyrimidin-2-amine
-
-
0.00053
N-(1-methylethyl)-4-(3-piperidin-3-yl-1H-pyrazol-4-yl)pyrimidin-2-amine
-
-
0.000162
N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
0.000381
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
0.000043
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
0.000169
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
0.000101
N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
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
0.000012
N-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
-
-
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
0.000028
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
-
-
0.000009
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
-
-
0.000012 - 0.000017
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
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
-
0.000023
(2S,3S)-2-[(R)-4-[4-(2-hydroxy-ethoxy)-phenyl]-2,5-dioxo-imidazolidin-1-yl]-3-phenyl-N-(4-propionyl-thiazol-2-yl)-butyramide
Homo sapiens
-
MEK1
0.000967
(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone
Homo sapiens
-
0.0000035
(R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide
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
-
0.05
1-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
larger than 0.050
0.05
2,2'-disulfanediylbis(1,3-benzothiazole)
Homo sapiens
-
-
0.000436
2-(benzyloxy)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine
Homo sapiens
-
0.00033
2-(ethylamino)-N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-1,3-thiazole-5-carboxamide
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
-
0.00031 - 0.00033
2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide
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
-
0.0000042
2-[(1-methylethyl)amino]-N-[2-methyl-5-(1H-pyrazol-5-ylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000035
2-[(1-methylethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000054
2-[(1-methylethyl)amino]-N-[2-methyl-5-[(1-methyl-1H-pyrazol-5-yl)carbamoyl]phenyl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.1
2-[(2,4-dinitrophenyl)sulfanyl]-1,3-benzoxazole
Homo sapiens
-
larger than 0.100
0.000022
2-[(2-methoxyethyl)amino]-N-[2-methyl-5-(methylcarbamoyl)phenyl]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0018
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
-
0.0027
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
Homo sapiens
-
-
0.0081
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
-
0.05
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole-5-sulfonic acid
Homo sapiens
-
larger than 0.050
0.0202
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-5-(trifluoromethyl)-1H-benzimidazole
Homo sapiens
-
-
0.0042
2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl][1,3]thiazolo[4,5-b]pyridine
Homo sapiens
-
-
0.000026
3-(3-bromo-4-[(2,4-difluorobenzyl)oxy]-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide
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
-
0.000209
3-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
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
-
0.0064 - 0.0071
3-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]benzamide
0.000061
3-[(4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridin-2-yl)amino]propan-1-ol
Homo sapiens
-
0.00011
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N,4-dimethylbenzamide
Homo sapiens
-
-
0.000053
3-[2-(cyclopropylamino)-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]-N-ethyl-4-methylbenzamide
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
-
0.00028 - 0.0005
4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-[(5-nitro-1,3,4-thiadiazol-2-yl)sulfanyl]-4H-1,2,4-triazol-3-ol
0.000002
4-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol
Homo sapiens
-
0.0018
4-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-2-carboxamide
Homo sapiens
-
0.1
4-[(1H-benzimidazol-2-ylsulfanyl)methyl]benzoic acid
Homo sapiens
-
larger than 0.100
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
-
0.00092
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-(1-methylethyl)pyrimidin-2-amine
Homo sapiens
-
-
0.0011
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclohexylpyrimidin-2-amine
Homo sapiens
-
-
0.00046
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopentylpyrimidin-2-amine
Homo sapiens
-
-
0.00084
4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-N-cyclopropylpyrimidin-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
-
0.07
4-[[(6-amino-9H-purin-8-yl)sulfanyl]methyl]benzoic acid
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
0.023
5,6-dichloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
-
0.00047 - 0.01
5-(5-nitrothiazol-2-ylthio)-N-((tetrahydrofuran-2-yl)methyl)-1,3,4-thiadiazol-2-amine
0.00029 - 0.0067
5-(5-nitrothiazol-2-ylthio)-N-propyl-1,3,4-thiadiazol-2-amine
0.0058 - 0.011
5-(acetylamino)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00026 - 0.00035
5-(difluoromethyl)-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.0032 - 0.0048
5-benzyl-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.0041 - 0.0099
5-bromo-N-(3-chloro-2-piperazin-1-ylphenyl)furan-2-carboxamide
0.00006 - 0.00009
5-bromo-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.02
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[2-(4-prop-2-en-1-ylpiperazin-1-yl)biphenyl-3-yl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[3-(phenylamino)-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.02
5-bromo-N-[3-bromo-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.00018 - 0.00096
5-bromo-N-[3-chloro-2-(4-cyclopropylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00036 - 0.0011
5-bromo-N-[3-chloro-2-(4-ethylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00036 - 0.0012
5-bromo-N-[3-chloro-2-(4-methylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00024 - 0.00033
5-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00014 - 0.00016
5-bromo-N-[3-chloro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00063 - 0.0009
5-bromo-N-[3-chloro-2-(4-propylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.001 - 0.0012
5-bromo-N-[3-chloro-2-(4-pyridin-2-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.0015 - 0.0022
5-bromo-N-[3-chloro-2-[4-(1-methylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0004 - 0.00054
5-bromo-N-[3-chloro-2-[4-(2-methylprop-2-en-1-yl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.0009 - 0.0014
5-bromo-N-[3-chloro-2-[4-(2-phenylethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.00025 - 0.00027
5-bromo-N-[3-chloro-2-[4-(furan-2-ylmethyl)piperazin-1-yl]phenyl]furan-2-carboxamide
0.02
5-bromo-N-[3-chloro-2-[4-(trifluoroacetyl)piperazin-1-yl]phenyl]furan-2-carboxamide
Homo sapiens
larger than 0.020
0.00011 - 0.00029
5-bromo-N-[3-fluoro-2-(4-prop-2-yn-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.00018 - 0.0002
5-bromo-N-[3-methyl-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]furan-2-carboxamide
0.05
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.027
5-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
Homo sapiens
-
-
0.00004 - 0.00008
5-chloro-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.00021 - 0.00023
5-cyano-N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]furan-2-carboxamide
0.0018
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
-
0.0047
5-methoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
-
0.0038
5-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
-
0.0064
5-nitro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole
Homo sapiens
-
-
0.000022
5-tert-butyl-N-cyclopropyl-2-methoxy-3-[2-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-2-oxo-acetylamino]-benzamide
Homo sapiens
-
-
0.0000004
6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)-N,N-dimethylphthalazin-1-amine
Homo sapiens
THP-1 cells
0.002
6-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyridine-2-carboxamide
Homo sapiens
-
0.05
6-chloro-2-[(4-methyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.05
6-chloro-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.05
6-chloro-2-[[4-(2,3-dihydro-1,4-benzodioxin-6-yl)-5-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.05
6-chloro-2-[[5-(2,4-dichlorophenyl)-4-methyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.05
6-chloro-2-[[5-(2-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
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
0.05
6-ethoxy-1,3-benzothiazole-2-sulfonamide
Homo sapiens
-
larger than 0.050
0.05
6-ethoxy-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzothiazole
Homo sapiens
-
larger than 0.050
0.05
6-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1,3-benzoxazole
Homo sapiens
-
larger than 0.050
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
0.055
6-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-2-amine
Homo sapiens
-
-
0.05
6-[5-[(6-chloro-1,3-benzothiazol-2-yl)sulfanyl]-4-methyl-4H-1,2,4-triazol-3-yl]quinoline
Homo sapiens
-
larger than 0.050
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
0.027
8-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-9H-purin-6-amine
Homo sapiens
-
-
0.000011 - 0.000079
BIRB 796
0.000035
BIRB796
Homo sapiens
-
-
0.000039
C2-alkylaminothiazole
Homo sapiens
-
inhibition of isozyme p38 MAPK alpha
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
0.00012
furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide
Homo sapiens
-
0.002 - 0.006
MKK4
-
0.3 - 0.4
MKK4 mutant F48K
-
0.003 - 0.045
MKK4 mutant L44I
-
0.00063
ML3375
Homo sapiens
-
0.00004
ML3403
Homo sapiens
-
0.00011
N,4-dimethyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
Homo sapiens
-
-
0.00027
N,4-dimethyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
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
-
0.00602
N-(1-methylethyl)-4-[3-(6-methylpyridin-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
Homo sapiens
-
-
0.0035
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
Homo sapiens
-
-
0.000357
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
Homo sapiens
-
-
0.000814
N-(1-methylethyl)-4-[3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]pyrimidin-2-amine
Homo sapiens
-
-
0.000221
N-(1-methylethyl)-4-[3-[1-(methylsulfonyl)piperidin-4-yl]-1H-pyrazol-4-yl]pyrimidin-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
-
0.000036
N-(2-chloro-6-methylphenyl)-2-(cyclobutylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.00014
N-(2-chloro-6-methylphenyl)-2-(ethylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.000062
N-(2-chloro-6-methylphenyl)-2-(phenylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.000028
N-(2-chloro-6-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.000013
N-(2-chloro-6-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.00016 - 0.0048
N-(2-methoxyethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.000126
N-(3,3-dimethylbutyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0001 - 0.0057
N-(3,4-dimethoxyphenethyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.000173
N-(4-fluorobenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0001 - 0.0091
N-(4-methoxybenzyl)-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
0.00134
N-(4-tert-butylbenzyl)-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-amine
Homo sapiens
-
0.0000041
N-(5-carbamoyl-2-methylphenyl)-2-(propylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000032
N-(5-carbamoyl-2-methylphenyl)-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
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
-
0.000245
N-cyclopentyl-4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-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
0.000034
N-ethyl-4-methyl-3-[2-[(1-methylethyl)amino]-6-oxo-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
Homo sapiens
-
-
0.00016
N-ethyl-4-methyl-3-[6-oxo-2-(propylamino)-4,6-dihydro-5H-pyrrolo[3,4-d][1,3]thiazol-5-yl]benzamide
Homo sapiens
-
-
0.0001 - 0.1
N-ethyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
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
0.00014 - 0.003
N-sec-butyl-5-(5-nitrothiazol-2-ylthio)-1,3,4-thiadiazol-2-amine
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
-
0.02
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-(phenylamino)furan-2-carboxamide
Homo sapiens
larger than 0.020
0.001 - 0.0014
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-ethylfuran-2-carboxamide
0.00021 - 0.00041
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-fluorofuran-2-carboxamide
0.00045 - 0.00062
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methoxyfuran-2-carboxamide
0.00033 - 0.00053
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-methylfuran-2-carboxamide
0.00011
N-[2-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)-3-methylphenyl]-5-prop-1-yn-1-ylfuran-2-carboxamide
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
-
0.0006 - 0.00081
N-[2-(4-acetylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.00088 - 0.0011
N-[2-(4-benzylpiperazin-1-yl)-3-chlorophenyl]-5-bromofuran-2-carboxamide
0.0000045
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000023
N-[2-methyl-5-(methylcarbamoyl)phenyl]-2-[[(1S)-1-methylpropyl]amino]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0023
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-4-carboxamide
Homo sapiens
-
0.0045 - 0.0089
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
0.0058
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-2-methyl-1,3-thiazole-4-carboxamide
Homo sapiens
-
0.02
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-5-cyanopyridine-2-carboxamide
Homo sapiens
larger than 0.020
0.0018 - 0.002
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-6-methylpyridine-2-carboxamide
0.005
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]isoxazole-5-carboxamide
Homo sapiens
-
0.02
N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]pyrimidine-2-carboxamide
Homo sapiens
larger than 0.020
0.000002
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-(propylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000034
N-[5-(ethylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.00013
N-[5-(ethylcarbamoyl)-2-methylphenyl]-4-methyl-2-(propylamino)-1,3-thiazole-5-carboxamide
Homo sapiens
-
-
0.0000038
N-[5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl]-2-[(1-methylethyl)amino]-1,3-thiazole-5-carboxamide
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
0.000299
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]acetamide
Homo sapiens
-
-
0.000114
N-[trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexyl]methanesulfonamide
Homo sapiens
-
-
0.05
S-1,3-benzothiazol-2-yl (2Z)-(2-amino-1,3-thiazol-4-yl)(methoxyimino)ethanethioate
Homo sapiens
-
larger than 0.050
0.00008 - 0.00015
SB 203580
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
0.000025
SR3451
Homo sapiens
-
-
0.000007
SR3576
Homo sapiens
-
-
0.000023
SR3582
Homo sapiens
-
-
0.00048
SR3583
Homo sapiens
-
-
0.0021
SR4018
Homo sapiens
-
-
0.00035
SR4276
Homo sapiens
-
-
0.000055
SR4326
Homo sapiens
-
-
0.0022
SR4642
Homo sapiens
-
-
0.0015
SR4643
Homo sapiens
-
-
0.0063 - 0.02
tert-butyl 4-(2-[[(5-bromofuran-2-yl)carbonyl]amino]-6-chlorophenyl)piperazine-1-carboxylate
0.000098
trans-4-([4-[3-(tetrahydro-2H-pyran-3-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)cyclohexanol
Homo sapiens
-
-
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
-
kinase assay
7.4
-
kinase assay
7.6
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
21
-
assay at room temperature
27
-
assay at
37
-
kinase assay
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
hepatoma cell line
Manually annotated by BRENDA team
from airway tissue
Manually annotated by BRENDA team
-
SV40 immortalized airway epithelial cell
Manually annotated by BRENDA team
-
urinary bladder cancer cells
Manually annotated by BRENDA team
highly expressed in
Manually annotated by BRENDA team
-
primary epithelial cells
Manually annotated by BRENDA team
-
cell line of a human with lymphoblastic leukemia
Manually annotated by BRENDA team
-
p38 isozymes alpha-delta expression patterns during erythroid differentiation of primary erythroid progenitors, isozymes alpha and gamma are expressed in early hematopoietic progenitors as well as in late differentiating erythroblasts, isozyme delta is only expressed and active during the terminal phase of erythroid differentiation, while isozyme beta is minimally expresses in early CD34+ hematopoietic progenitors
Manually annotated by BRENDA team
-
mesothelioma cell line
Manually annotated by BRENDA team
-
the MAPK family enzymes have regulatory function in the myocardium
Manually annotated by BRENDA team
-
207 different sources, MAPK expression and immunohistochemical analysis, mutational analysis of up-regulating kinases BRAF and KRAS
Manually annotated by BRENDA team
highly expressed in
Manually annotated by BRENDA team
-
lesional psoriatic skin
Manually annotated by BRENDA team
-
of airway and alveolar endothelium
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
additional information
-
CAD occurs in the cytoplasm and the nucleus, but is phosphorylated only in the nucleus, CAD translocation is induced by EGF stimulation
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
metabolism
mycosporine-like amino acids promote wound healing through focal adhesion kinase (FAK, EC 2.7.10.2) and mitogen-activated protein kinases (MAP kinases) signaling pathway in keratinocytes
physiological function
essential role of mitogen-activated protein kinases in IL-17A-induced matrix metalloproteinase MMP-3 expression in human synovial sarcoma cells, overview. IL-17A induces MMP-1 and MMP-9 via ERK1/2 and p38 MAPK-dependent activation of the transcriptional factors activator protein-1 (AP-1) and nuclear factor-kappa B (NF-kappaB)
malfunction
metabolism
physiological function
additional information
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
MK03_HUMAN
379
0
43136
Swiss-Prot
other Location (Reliability: 1)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
45000
-
JNK1
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 43472-43556, unphosphorylated to trifold phosphorylated p38 MAPKalpha, mass spectrometry
dimer
-
phosphorylated ERK2 using gel filtration, SAPKRI/JNK2 using sedimentation analysis
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
phosphoprotein
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
crystal structure of p38alpha, show docking grooves for binding of substrate D-domains, i.e. of MEF2A, and of activating kinases, e.g. of MKK3b, Ile116 and Gln120 play important roles
crystal structure of the unphosphorylated p38alpha-MK2, by hanging drop method, full-length p38alpha-MK2 complex to 4 A resolution, belongs to spacegroup P41 with unit cell dimensions of 103.09 A, 103.09 A, 231.42 A, 90.0°, 90.0°, 90.0°, p38alpha-MK2 peptide complex, belongs to spacegroup P31 with unit cell dimensions of 81.55 A, 81.55 A, 121.36 A, 90.0°, 90.0°, 120.0°. C-terminal regulatory domain of MK2 binds in the docking groove of p38alpha, and the ATP-binding sites of both kinases are at the heterodimer interface
-
isolated PDZ domain of protein tyrosine phosphatase non-receptor type bound to the p38gamma C-terminus, i.e. Cyto8-RETEV and p38gamma-KETPL peptides, mixing of the protein ligand solution from 5 mg/ml PTPN4-PDZ domain and the appropriate peptide at a ratio of 1:2 and 1:4 for PTPN4-PDZCyto8-RETEV and PTPN4-PDZp38gamma-KETPL, respectively, in 50 mM Tris-HCl, pH 7.5, 150 mM NaCl, 0.5 mM TCEP, sitting drop vapor diffusion method, mixing of 400 nl protein-ligand solution with 200 nl of precipitant solution containing 23% PEG 8000, 100 mM MES, pH 6.0, 200 mM calcium acetate, 0.143 mM ammonium sulfate or 1.2 M sodium dihydrogen phosphate, 0.8 M dipotassium hydrogen phosphate, 0.1 M CAPS, pH 10.5, 0.2 M lithium sulfate, 0.67 M non-detergent sulfobetaine (NDSB) 201, 18°C, X-ray diffraction structure determination and analysis at 2.09-2.35 A resolution, modeling
purified recombinant His-tagged mutant enzyme in complex with inhibitor furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide in 0.1 M MES, pH5.6, and 0.88 M sodium citrate, mixing of 0.001 ml of protein in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2, 5% glycerol, 5 mM DTT, and 0.02% octyl-beta-D-glucopyranoside with 0.001 ml of 0.1 M MES, pH 5.6, 0.56-0.62 M sodium citrate, and 500 nl of 1000fold diluted seed stock, X-ray diffraction structure determination and analysis at 2.15 A resolution, molecular replacment and modelling
the structure of SR3737 and SR3451-soaked JNK3 crystals are solved at 2.20 and 2.29 A, respectively
-
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
C177S/C222S/K250A/K251A/K265A/K270A
site-directed mutagenesis, the hexa-surfaced mutant forms crystallization complexes with inhibitor furan-2-carboxylic acid (3-[5-(4H-[1,2,4]triazol-3-yl)-1H-indazol-3-yl]-phenyl)-amide in contrast to other mutant variants or the wild-type enzyme
D176A
site-directed mutagenesis of p38beta, 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
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
D3K/C6V/S8N/14E
site-directed mutagenesis using JNK2 1-362 or 1-364, the mutant does not crystallize
E339A
-
in 100 mM KCl completely dimeric
F329A
-
retains ability to dimerize significantly in 100 mM KCl
H176A/F181A/L4A
-
retains ability to dimerize significantly in 100 mM KCl
H176E
-
retains ability to dimerize significantly in 100 mM KCl
H176E/E343A
-
retains ability to dimerize significantly in 100 mM KCl
H176E/L2E/E343A
-
retains ability to dimerize significantly in 100 mM KCl
H176E/L4A
-
in 100 mM KCl almost completely monomeric
K203A/E204A
site-directed mutagenesis, the mutant does not crystallize
K340A
-
in 100 mM KCl completely dimeric
K340E/L3E
-
retains ability to dimerize significantly in 100 mM KCl
K53A
-
kinase-negative mutant
L2E
-
in 100 mM KCl completely dimeric
L4A
-
retains ability to dimerize significantly in 100 mM KCl
T106M
-
inhibitor-insensitive mutant
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
a SP Fastflow column, a Mono S column, and a Sephacryl S200 column are used
-
gel filtration
-
glutathione-Sepharose column chromatography
-
GST- and His-tags are used in the purification experiments
-
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
recombinant His-tagged p38 isozyme alpha from Escherichia coli strain BL21(DE3) by nickel affinity and ion exchange chromatography to over 98% purity, removal of the His-tag by thrombin is required for propper enzyme purification and activation
-
recombinant wild-type and mutant enzymes from Escherichia coli strain BL21(DE3) by anion exchange chromatography and gel filtration for non-tagged proteins, His6-tagged proteins are purified by nickel affinity chromatography
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
expressed in Escherichia coli as a glutathione S-transferase fusion protein
isolation of cDNA
a pDEST_JNK3_39-402 construct is used for the expression of the protein in Escherichia coli BL21DE3 cells
-
a plasmid encoding Flag-JNK1 is used
-
characterization of cDNA
expressed in CHO/KOR cells
-
expressed in Escherichia coli BL21(DE3) cells
-
expression of ERK in CHO cells, co-expression of serotonin 5-HT2c receptor leads to increased ERK phosphorylation
-
expression of His-tagged isozyme p38alpha MAPK in Escherichia coli
expression of His-tagged p38 isozyme alpha in Escherichia coli strain BL21(DE3)
-
expression of wild-type and mutant enzymes with or without His6-tag in Escherichia coli strain BL21(DE3)
heterogeneous expression in different tissues
into the plasmid pRSET-CA for expression in Escherichia coli Bl21DE3 cells
-
mutated fragments of ERK2 subcloned into wild-type or mutated forms of the bacterial coexpression system plasmid, R4FMEK1 plus ERK2pETHis6. SAPKalphaI/JNK2 expressed from pRSETSAPKalphaI and from the bacterial coexpression system
-
recombinant expression of C-terminally His6-tagged p38alpha in Escherichia coli strain BL21 (DE3) RIL
recombinant expression of GST-tagged enzyme
transient expression of wild-type and mutant p38alpha in HEK-293 cells
transient expression of wild-type and mutant p38beta in HEK-293 cells
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
0.2 mM 6-nitro-7-sulfamoylbenzoquinoxaline decreases both p-ERK1/2 and p-Src Tyr416 levels in a time-dependent manner
-
0.2 mM alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid increases both p-ERK1/2 and p-Src Tyr416 levels in a time-dependent manner
-
JNK activity is elevated in adipocytes of type 2 diabetic patients
-
Porphyromonas gingivalis supernatant up-regulates ERK1/2 expression
-
Porphyromonas gingivalis supernatant up-regulates JNK expression
-
Porphyromonas gingivalis supernatant up-regulates p38 expression
-
the MAPK pathway is often up-regulated in cancers
-
up-regulation of JNK activity is associated with a number of disease states such as type-2 diabetes, obesity, cancer, inflammation, and stroke
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine
the inhibitors of Erk1 or antioxidants may be exploited for prevention of cadmium-induced neurodegenerative diseases
analysis
drug development
medicine
pharmacology
-
MAPKs are targets for inhibitors and pharmacological drug development
additional information
-
phosphorylated ERK2 has an increased capacity to form dimers relative to unphosphorylated ERK2, dimerization of SAPKalphaI/JNK2 displays no dependence on phosphorylation
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Dunham, I.; Shimizu, N.; Roe, B.A.; Chissoe, S.; Hunt, A.R.; Collins, J.E.; Bruskiewich, R.; Beare, D.M.; Clamp, M.; Smink, L.J.; Ainscough, R.; Almeida, J.P.; Babbage, A.; Bagguley, C.; Bailey, J.; Barlow, K.; Bates, K.N.; Beasley, O.; Bird, C.P.; Blakey, S.; Bridgeman, A.M.; Buck, D.; Burgess, J.; Burrill, W.D.; O'Brien, K.P.; et al.
The DNA sequence of human chromosome 22
Nature
402
489-495
1999
Homo sapiens (Q15759)
Manually annotated by BRENDA team
Knebel, A.; Morrice, N.; Cohen, P.
A novel method to identify protein kinase substrates: eEF2 kinase is phosphorylated and inhibited by SAPK4/p38delta
EMBO J.
20
4360-4369
2001
Homo sapiens (O15264)
Manually annotated by BRENDA team
Hu, M.C.; Wang, Y.P.; Mikhail, A.; Qiu, W.R.; Tan, T.H.
Murine p38-delta mitogen-activated protein kinase, a developmentally regulated protein kinase that is activated by stress and proinflammatory cytokines
J. Biol. Chem.
274
7095-7102
1999
Homo sapiens (O15264), Homo sapiens, Rattus norvegicus (Q9WTY9)
Manually annotated by BRENDA team
Herbison, C.E.; Sayer, D.C.; Bellgard, M.; Allcock, R.J.; Christiansen, F.T.; Price, P.
Structure and polymorphism of two stress-activated protein kinase genes centromeric of the MH: SAPK2a and SAPK4
DNA Seq.
10
229-243
1999
Homo sapiens (O15264), Homo sapiens, Pan troglodytes (Q95NE7), Pan troglodytes (Q9N272), Pan troglodytes
Manually annotated by BRENDA team
Hale, K.K.; Trollinger, D.; Rihanek, M.; Manthey, C.L.
Differential expression and activation of p38 mitogen-activated protein kinase alpha, beta, gamma, and delta in inflammatory cell lineages
J. Immunol.
162
4246-4252
1999
Homo sapiens (O15264)
Manually annotated by BRENDA team
Wang, X.S.; Diener, K.; Manthey, C.L.; Wang, S.; Rosenzweig, B.; Bray, J.; Delaney, J.; Cole, C.N.; Chan-Hui, P.Y.; Mantlo, N.; Lichenstein, H.S.; Zukowski, M.; Yao, Z.
Molecular cloning and characterization of a novel p38 mitogen-activated protein kinase
J. Biol. Chem.
272
23668-23674
1997
Homo sapiens (O15264), Homo sapiens
Manually annotated by BRENDA team
Kumar, S.; McDonnell, P.C.; Gum, R.J.; Hand, A.T.; Lee, J.C.; Young, P.R.
Novel homologues of CSBP/p38 MAP kinase: activation, substrate specificity and sensitivity to inhibition by pyridinyl imidazoles
Biochem. Biophys. Res. Commun.
235
533-538
1997
Homo sapiens (O15264), Homo sapiens (Q15759)
Manually annotated by BRENDA team
Jiang, Y.; Gram, H.; Zhao, M.; New, L.; Gu, J.; Feng, L.; Di Padova, F.; Ulevitch, R.J.; Han, J.
Characterization of the structure and function of the fourth member of p38 group mitogen-activated protein kinases, p38delta
J. Biol. Chem.
272
30122-30128
1997
Homo sapiens (O15264)
Manually annotated by BRENDA team
Goedert, M.; Cuenda, A.; Craxton, M.; Jakes, R.; Cohen, P.
Activation of the novel stress-activated protein kinase SAPK4 by cytokines and cellular stresses is mediated by SKK3 (MKK6); comparison of its substrate specificity with that of other SAP kinases
EMBO J.
16
3563-3571
1997
Homo sapiens (O15264), Homo sapiens (Q15759), Homo sapiens
Manually annotated by BRENDA team
Charest, D.L.; Mordret, G.; Harder, K.W.; Jirik, F.; Pelech, S.L.
Molecular cloning, expression, and characterization of the human mitogen-activated protein kinase p44erk1
Mol. Cell. Biol.
13
4679-4690
1993
Homo sapiens (P27361), Homo sapiens
Manually annotated by BRENDA team
Owaki, H.; Makar, R.; Boulton, T.G.; Cobb, M.H.; Geppert, T.D.
Extracellular signal-regulated kinases in T cells: characterization of human ERK1 and ERK2 cDNAs
Biochem. Biophys. Res. Commun.
182
1416-1422
1992
Homo sapiens (P27361), Homo sapiens (P28482), Homo sapiens
Manually annotated by BRENDA team
Gonzalez, F.A.; Raden, D.L.; Rigby, M.R.; Davis, R.J.
Heterogeneous expression of four MAP kinase isoforms in human tissues
FEBS Lett.
304
170-178
1992
Schizosaccharomyces pombe (P27638), Homo sapiens (P28482), Homo sapiens (P31152), Homo sapiens
Manually annotated by BRENDA team
Fleming, Y.; Armstrong, C.G.; Morrice, N.; Paterson, A.; Goedert, M.; Cohen, P.
Synergistic activation of stress-activated protein kinase 1/c-Jun N-terminal kinase (SAPK1/JNK) isoforms by mitogen-activated protein kinase kinase 4 (MKK4) and MKK7
Biochem. J.
352
145-154
2000
Homo sapiens (P45983), Homo sapiens (P45984)
-
Manually annotated by BRENDA team
Gupta, S.; Barrett, T.; Whitmarsh, A.J.; Cavanagh, J.; Sluss, H.K.; Derijard, B.; Davis, R.J.
Selective interaction of JNK protein kinase isoforms with transcription factors
EMBO J.
15
2760-2770
1996
Homo sapiens (P45983), Homo sapiens (P45984), Homo sapiens (P53779), Homo sapiens
Manually annotated by BRENDA team
Derijard, B.; Raingeaud, J.; Barrett, T.; Wu, I.H.; Han, J.; Ulevitch, R.J.; Davis, R.J.
Independent human MAP-kinase signal transduction pathways defined by MEK and MKK isoforms
Science
267
682-685
1995
Homo sapiens (P45983), Homo sapiens, Mus musculus (P47811)
Manually annotated by BRENDA team
Derijard, B.; Hibi, M.; Wu, I.H.; Barrett, T.; Su, B.; Deng, T.; Karin, M.; Davis, R.J.
JNK1: a protein kinase stimulated by UV light and Ha-Ras that binds and phosphorylates the c-Jun activation domain
Cell
76
1025-1037
1994
Homo sapiens (P45983)
Manually annotated by BRENDA team
Sluss, H.K.; Barrett, T.; Derijard, B.; Davis, R.J.
Signal transduction by tumor necrosis factor mediated by JNK protein kinases
Mol. Cell. Biol.
14
8376-8384
1994
Homo sapiens (P45984)
Manually annotated by BRENDA team
Kallunki, T.; Su, B.; Tsigelny, I.; Sluss, H.K.; Derijard, B.; Moore, G.; Davis, R.; Karin, M.
JNK2 contains a specificity-determining region responsible for efficient c-Jun binding and phosphorylation
Genes Dev.
8
2996-3007
1994
Homo sapiens (P45984)
Manually annotated by BRENDA team
Mohit, A.A.; Martin, J.H.; Miller, C.A.
P493F12 kinase: a novel MAP kinase expressed in a subset of neurons in the human nervous system
Neuron
14
67-78
1995
Homo sapiens (P53779), Homo sapiens
Manually annotated by BRENDA team
Zhou, G.; Bao, Z.Q.; Dixon, J.E.
Components of a new human protein kinase signal transduction pathway
J. Biol. Chem.
270
12665-12669
1995
Homo sapiens (Q13164), Homo sapiens
Manually annotated by BRENDA team
Lee, J.D.; Ulevitch, R.J.; Han, J.
Primary structure of BMK1: a new mammalian map kinase
Biochem. Biophys. Res. Commun.
213
715-724
1995
Homo sapiens (Q13164), Homo sapiens
Manually annotated by BRENDA team
Enslen, H.; Raingeaud, J.; Davis, R.J.
Selective activation of p38 mitogen-activated protein (MAP) kinase isoforms by the MAP kinase kinases MKK3 and MKK6
J. Biol. Chem.
273
1741-1748
1998
Homo sapiens (Q15759)
Manually annotated by BRENDA team
Stein, B.; Yang, M.X.; Young, D.B.; Janknecht, R.; Hunter, T.; Murray, B.W.; Barbosa, M.S.
P38-2, a novel mitogen-activated protein kinase with distinct properties
J. Biol. Chem.
272
19509-19517
1997
Homo sapiens (Q15759)
Manually annotated by BRENDA team
Jiang, Y.; Chen, C.; Li, Z.; Guo, W.; Gegner, J.A.; Lin, S.; Han, J.
Characterization of the structure and function of a new mitogen-activated protein kinase (p38beta)
J. Biol. Chem.
271
17920-17926
1996
Homo sapiens (Q15759), Homo sapiens
Manually annotated by BRENDA team
Meloche, S.; Beatty, B.G.; Pellerin, J.
Primary structure, expression and chromosomal locus of a human homolog of rat ERK3
Oncogene
13
1575-1579
1996
Homo sapiens (Q16659), Homo sapiens
Manually annotated by BRENDA team
Zhu, A.X.; Zhao, Y.; Moller, D.E.; Flier, J.S.
Cloning and characterization of p97MAPK, a novel human homolog of rat ERK-3
Mol. Cell. Biol.
14
8202-8211
1994
Homo sapiens (Q16659), Homo sapiens
Manually annotated by BRENDA team
Bain, J.; McLauchlan, H.; Elliott, M.; Cohen, P.
The specificities of protein kinase inhibitors: an update
Biochem. J.
371
199-204
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Biondi, R.M.; Nebreda, A.R.
Signalling specificity of Ser/Thr protein kinases through docking-site-mediated interactions
Biochem. J.
372
1-13
2003
Homo sapiens (P53778)
Manually annotated by BRENDA team
Ratner, A.J.; Bryan, R.; Weber, A.; Nguyen, S.; Barnes, D.; Pitt, A.; Gelber, S.; Cheung, A.; Prince, A.
Cystic fibrosis pathogens activate Ca2+-dependent mitogen-activated protein kinases signaling pathways in airway epithelial cells
J. Biol. Chem.
276
19267-19275
2001
Homo sapiens
Manually annotated by BRENDA team
Werry, T.D.; Gregory, K.J.; Sexton, P.M.; Christopoulos, A.
Characterization of serotonin 5-HT2C receptor signaling to extracellular signal-regulated kinases 1 and 2
J. Neurochem.
93
1603-1615
2005
Homo sapiens
Manually annotated by BRENDA team
Szafranska, A.E.; Luo, X.; Dalby, K.N.
Following in vitro activation of mitogen-activated protein kinases by mass spectrometry and tryptic peptide analysis: purifying fully activated p38 mitogen-activated protein kinase alpha
Anal. Biochem.
336
1-10
2005
Homo sapiens
Manually annotated by BRENDA team
Hofmann, M.; Zaper, J.; Bernd, A.; Bereiter-Hahn, J.; Kaufmann, R.; Kippenberger, S.
Mechanical pressure-induced phosphorylation of p38 mitogen-activated protein kinase in epithelial cells via Src and protein kinase C
Biochem. Biophys. Res. Commun.
316
673-679
2004
Homo sapiens
Manually annotated by BRENDA team
Tudan, C.; Jackson, J.K.; Higo, T.T.; Hampong, M.; Pelech, S.L.; Burt, H.M.
Calcium pyrophosphate dihydrate crystal associated induction of neutrophil activation and repression of TNF-alpha-induced apoptosis is mediated by the p38 MAP kinase
Cell. Signal.
16
211-221
2004
Homo sapiens
Manually annotated by BRENDA team
Hsu, C.Y.; Bristow, R.; Cha, M.S.; Wang, B.G.; Ho, C.L.; Kurman, R.J.; Wang, T.L.; Shih Ie, M.
Characterization of active mitogen-activated protein kinase in ovarian serous carcinomas
Clin. Cancer Res.
10
6432-6436
2004
Homo sapiens
Manually annotated by BRENDA team
Pelaia, G.; Cuda, G.; Vatrella, A.; Fratto, D.; Tagliaferri, P.; Maselli, R.; Costanzo, F.S.; Marsico, S.A.
Mitogen-activated protein kinases: new molecular targets for pharmacological treatment of inflammatory lung diseases
Curr. Med. Chem.
2
131-141
2003
Homo sapiens
-
Manually annotated by BRENDA team
Sigoillot, F.D.; Kotsis, D.H.; Serre, V.; Sigoillot, S.M.; Evans, D.R.; Guy, H.I.
Nuclear localization and mitogen-activated protein kinase phosphorylation of the multifunctional protein CAD
J. Biol. Chem.
280
25611-25620
2005
Homo sapiens, Mesocricetus auratus
Manually annotated by BRENDA team
Ravingerova, T.; Barancik, M.; Strniskova, M.
Mitogen-activated protein kinases: a new therapeutic target in cardiac pathology
Mol. Cell. Biochem.
247
127-138
2003
Canis lupus familiaris, Oryctolagus cuniculus, Homo sapiens, Mus musculus, Rattus norvegicus, Sus scrofa
Manually annotated by BRENDA team
Miller, A.L.; Webb, M.S.; Copik, A.J.; Wang, Y.; Johnson, B.H.; Kumar, R.; Thompson, E.B.
p38 Mitogen-activated protein kinase (MAPK) is a key mediator in glucocorticoid-induced apoptosis of lymphoid cells: correlation between p38 MAPK activation and site-specific phosphorylation of the human glucocorticoid receptor at serine 211
Mol. Endocrinol.
19
1569-1583
2005
Homo sapiens
Manually annotated by BRENDA team
Uddin, S.; Ah-Kang, J.; Ulaszek, J.; Mahmud, D.; Wickrema, A.
Differentiation stage-specific activation of p38 mitogen-activated protein kinase isoforms in primary human erythroid cells
Proc. Natl. Acad. Sci. USA
101
147-152
2004
Homo sapiens
Manually annotated by BRENDA team
Zaman, G.J.; van der Lee, M.M.; Kok, J.J.; Nelissen, R.L.; Loomans, E.E.
Enzyme fragment complementation binding assay for p38alpha mitogen-activated protein kinase to study the binding kinetics of enzyme inhibitors
Assay Drug Dev. Technol.
4
411-420
2006
Homo sapiens
Manually annotated by BRENDA team
Wilsbacher, J.L.; Juang, Y.C.; Khokhlatchev, A.V.; Gallagher, E.; Binns, D.; Goldsmith, E.J.; Cobb, M.H.
Characterization of mitogen-activated protein kinase (MAPK) dimers
Biochemistry
45
13175-13182
2006
Homo sapiens
Manually annotated by BRENDA team
Champelovier, P.; El Atifi, M.; Pautre, V.; Rostaing, B.; Berger, F.; Seigneurin, D.
Specific inhibition of basal mitogen-activated protein kinases and phosphatidylinositol 3 kinase activities in leukemia cells: a possible therapeutic role for the kinase inhibitors
Exp. Hematol.
36
28-36
2007
Homo sapiens
Manually annotated by BRENDA team
ter Haar, E.; Prabhakar, P.; Prabakhar, P.; Liu, X.; Lepre, C.
Crystal structure of the p38 alpha-MAPKAP kinase 2 heterodimer
J. Biol. Chem.
282
9733-9739
2007
Homo sapiens
Manually annotated by BRENDA team
Tao, X.; Tong, L.
Crystal structure of the MAP kinase binding domain and the catalytic domain of human MKP5
Protein Sci.
16
880-886
2007
Homo sapiens
Manually annotated by BRENDA team
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
Hynes, J.; Wu, H.; Pitt, S.; Shen, D.R.; Zhang, R.; Schieven, G.L.; Gillooly, K.M.; Shuster, D.J.; Taylor, T.L.; Yang, X.; McIntyre, K.W.; McKinnon, M.; Zhang, H.; Marathe, P.H.; Doweyko, A.M.; Kish, K.; Kiefer, S.E.; Sack, J.S.; Newitt, J.A.; Barrish, J.C.; Dodd, J.; Leftheris, K.
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor
Bioorg. Med. Chem. Lett.
18
1762-1767
2008
Homo sapiens
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
Montalban, A.G.; Boman, E.; Chang, C.D.; Ceide, S.C.; Dahl, R.; Dalesandro, D.; Delaet, N.G.; Erb, E.; Gibbs, A.; Kahl, J.; Kessler, L.; Lundstroem, J.; Miller, S.; Nakanishi, H.; Roberts, E.; Saiah, E.; Sullivan, R.; Wang, Z.; Larson, C.J.
Reverse alpha-ketoamide-based p38 MAP kinase inhibitors
Bioorg. Med. Chem. Lett.
18
5456-5459
2008
Homo sapiens
Manually annotated by BRENDA team
Chen, L.; Liu, L.; Huang, S.
Cadmium activates the mitogen-activated protein kinase (MAPK) pathway via induction of reactive oxygen species and inhibition of protein phosphatases 2A and 5
Free Radic. Biol. Med.
45
1035-1044
2008
Homo sapiens, Homo sapiens (P27361), Homo sapiens (P28482), Rattus norvegicus, Rattus norvegicus (P21708), Rattus norvegicus (P63086)
Manually annotated by BRENDA team
Lee, S.J.; Park, S.S.; Lee, U.S.; Kim, W.J.; Moon, S.K.
Signaling pathway for TNF-alpha-induced MMP-9 expression: Mediation through p38 MAP kinase, and inhibition by anti-cancer molecule magnolol in human urinary bladder cancer 5637 cells
Int. Immunopharmacol.
8
1821-1826
2008
Homo sapiens
Manually annotated by BRENDA team
Liu, W.; Liang, Q.; Balzar, S.; Wenzel, S.; Gorska, M.; Alam, R.
Cell-specific activation profile of extracellular signal-regulated kinase 1/2, Jun N-terminal kinase, and p38 mitogen-activated protein kinases in asthmatic airways
J. Allergy Clin. Immunol.
121
893-902.e2
2008
Homo sapiens (P27361), Homo sapiens (P28482), Homo sapiens
Manually annotated by BRENDA team
Binet, F.; Girard, D.
Novel human neutrophil agonistic properties of arsenic trioxide: involvement of p38 mitogen-activated protein kinase and/or c-jun NH2-terminal MAPK but not extracellular signal-regulated kinases-1/2
J. Leukoc. Biol.
84
1613-1622
2008
Homo sapiens
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
Shaw, D.; Wang, S.M.; Villasenor, A.G.; Tsing, S.; Walter, D.; Browner, M.F.; Barnett, J.; Kuglstatter, A.
The crystal structure of JNK2 reveals conformational flexibility in the MAP kinase insert and indicates its involvement in the regulation of catalytic activity
J. Mol. Biol.
383
885-893
2008
Homo sapiens (P45984), Homo sapiens
Manually annotated by BRENDA team
Chang, C.H.; Yu, F.Y.; Wang, L.T.; Lin, Y.S.; Liu, B.H.
Activation of ERK and JNK signaling pathways by mycotoxin citrinin in human cells
Toxicol. Appl. Pharmacol.
237
281-287
2009
Homo sapiens
Manually annotated by BRENDA team
Kawai, K.; Saito, A.; Sudo, T.; Osada, H.
A p38 mitogen-activated protein kinase inhibitor screening method using growth recovery of Escherichia coli as an index
Anal. Biochem.
388
128-133
2009
Homo sapiens
Manually annotated by BRENDA team
Yanti, H.K.; Lee, M.; Kim, D.; Hwang, J.K.
Inhibitory effect of panduratin A on c-Jun N-terminal kinase and activator protein-1 signaling involved in Porphyromonas gingivalis supernatant-stimulated matrix metalloproteinase-9 expression in human oral epidermoid cells
Biol. Pharm. Bull.
32
1770-1775
2009
Homo sapiens
Manually annotated by BRENDA team
Humphries, P.S.; Lafontaine, J.A.; Agree, C.S.; Alexander, D.; Chen, P.; Do, Q.Q.; Li, L.Y.; Lunney, E.A.; Rajapakse, R.J.; Siegel, K.; Timofeevski, S.L.; Wang, T.; Wilhite, D.M.
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors
Bioorg. Med. Chem. Lett.
19
2099-2102
2009
Homo sapiens
Manually annotated by BRENDA team
Shin, Y.; Chen, W.; Habel, J.; Duckett, D.; Ling, Y.Y.; Koenig, M.; He, Y.; Vojkovsky, T.; LoGrasso, P.; Kamenecka, T.M.
Synthesis and SAR of piperazine amides as novel c-jun N-terminal kinase (JNK) inhibitors
Bioorg. Med. Chem. Lett.
19
3344-3347
2009
Homo sapiens, Homo sapiens (P53779)
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
De, S.K.; Chen, L.H.; Stebbins, J.L.; Machleidt, T.; Riel-Mehan, M.; Dahl, R.; Chen, V.; Yuan, H.; Barile, E.; Emdadi, A.; Murphy, R.; Pellecchia, M.
Discovery of 2-(5-nitrothiazol-2-ylthio)benzo[d]thiazoles as novel c-Jun N-terminal kinase inhibitors
Bioorg. Med. Chem.
17
2712-2717
2009
Homo sapiens
Manually annotated by BRENDA team
De, S.K.; Chen, V.; Stebbins, J.L.; Chen, L.H.; Cellitti, J.F.; Machleidt, T.; Barile, E.; Riel-Mehan, M.; Dahl, R.; Yang, L.; Emdadi, A.; Murphy, R.; Pellecchia, M.
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors
Bioorg. Med. Chem.
18
590-596
2010
Homo sapiens
Manually annotated by BRENDA team
Soegaard-Madsen, L.; Johansen, C.; Iversen, L.; Kragballe, K.
Adalimumab therapy rapidly inhibits p38 mitogen-activated protein kinase activity in lesional psoriatic skin preceding clinical improvement
Br. J. Dermatol.
162
1216-1223
2010
Homo sapiens
Manually annotated by BRENDA team
Daouti, S.; Wang, H.; Li, W.H.; Higgins, B.; Kolinsky, K.; Packman, K.; Specian, A.; Kong, N.; Huby, N.; Wen, Y.; Xiang, Q.; Podlaski, F.J.; He, Y.; Fotouhi, N.; Heimbrook, D.; Niu, H.
Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy
Cancer Res.
69
1924-1932
2009
Homo sapiens
Manually annotated by BRENDA team
Chung, E.J.; Brown, A.P.; Asano, H.; Mandler, M.; Burgan, W.E.; Carter, D.; Camphausen, K.; Citrin, D.
In vitro and in vivo radiosensitization with AZD6244 (ARRY-142886), an inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase 1/2 kinase
Clin. Cancer Res.
15
3050-3057
2009
Homo sapiens
Manually annotated by BRENDA team
Beretta, F.; Bassani, S.; Binda, E.; Verpelli, C.; Bello, L.; Galli, R.; Passafaro, M.
The GluR2 subunit inhibits proliferation by inactivating Src-MAPK signalling and induces apoptosis by means of caspase 3/6-dependent activation in glioma cells
Eur. J. Neurosci.
30
25-34
2009
Homo sapiens
Manually annotated by BRENDA team
Montalban, A.G.; Boman, E.; Chang, C.D.; Ceide, S.C.; Dahl, R.; Dalesandro, D.; Delaet, N.G.; Erb, E.; Ernst, J.; Gibbs, A.; Kahl, J.; Kessler, L.; Lundstroem, J.; Miller, S.; Nakanishi, H.; Roberts, E.; Saiah, E.; Sullivan, R.; Wang, Z.; Larson, C.J.
KR-003048, a potent, orally active inhibitor of p38 mitogen-activated protein kinase
Eur. J. Pharmacol.
632
93-102
2010
Homo sapiens
Manually annotated by BRENDA team
Yao, K.; Cho, Y.Y.; Bode, A.M.; Vummenthala, A.; Park, J.G.; Liu, K.; Pang, Y.P.; Dong, Z.
A selective small-molecule inhibitor of c-Jun N-terminal kinase 1
FEBS Lett.
583
2208-2212
2009
Mus musculus, Homo sapiens (P45983)
Manually annotated by BRENDA team
Kamenecka, T.; Habel, J.; Duckett, D.; Chen, W.; Ling, Y.Y.; Frackowiak, B.; Jiang, R.; Shin, Y.; Song, X.; LoGrasso, P.
Structure-activity relationships and X-ray structures describing the selectivity of aminopyrazole inhibitors for c-Jun N-terminal kinase 3 (JNK3) over p38
J. Biol. Chem.
284
12853-12861
2009
Homo sapiens, Mammalia
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
Aronov, A.M.; Tang, Q.; Martinez-Botella, G.; Bemis, G.W.; Cao, J.; Chen, G.; Ewing, N.P.; Ford, P.J.; Germann, U.A.; Green, J.; Hale, M.R.; Jacobs, M.; Janetka, J.W.; Maltais, F.; Markland, W.; Namchuk, M.N.; Nanthakumar, S.; Poondru, S.; Straub, J.; ter Haar, E.; Xie, X.
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control
J. Med. Chem.
52
6362-6368
2009
Homo sapiens (P28482), Homo sapiens
Manually annotated by BRENDA team
Ohba, S.; Hirose, Y.; Kawase, T.; Sano, H.
Inhibition of c-Jun N-terminal kinase enhances temozolomide-induced cytotoxicity in human glioma cells
J. Neurooncol.
95
307-316
2009
Homo sapiens
Manually annotated by BRENDA team
Hope, H.R.; Anderson, G.D.; Burnette, B.L.; Compton, R.P.; Devraj, R.V.; Hirsch, J.L.; Keith, R.H.; Li, X.; Mbalaviele, G.; Messing, D.M.; Saabye, M.J.; Schindler, J.F.; Selness, S.R.; Stillwell, L.I.; Webb, E.G.; Zhang, J.; Monahan, J.B.
Anti-inflammatory properties of a novel N-phenyl pyridinone inhibitor of p38 mitogen-activated protein kinase: preclinical-to-clinical translation
J. Pharmacol. Exp. Ther.
331
882-895
2009
Homo sapiens
Manually annotated by BRENDA team
Onali, P.; Dedoni, S.; Olianas, M.C.
Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes
J. Pharmacol. Exp. Ther.
332
255-265
2010
Homo sapiens, Rattus norvegicus
Manually annotated by BRENDA team
da Costa, S.V.; Roela, R.A.; Junqueira, M.S.; Arantes, C.; Brentani, M.M.
The role of p38 mitogen-activated protein kinase in serum-induced leukemia inhibitory factor secretion by bone marrow stromal cells from pediatric myelodysplastic syndromes
Leuk. Res.
34
507-512
2010
Homo sapiens
Manually annotated by BRENDA team
Chai, B.; Li, J.Y.; Zhang, W.; Wang, H.; Mulholland, M.W.
Melanocortin-4 receptor activation inhibits c-Jun N-terminal kinase activity and promotes insulin signaling
Peptides
30
1098-1104
2009
Homo sapiens
Manually annotated by BRENDA team
Faugaret, D.; Dauba, A.; Baron, C.; Velge-Roussel, F.; Lebranchu, Y.
Mycophenolic acid inhibits p38 mitogen-activated protein kinase in human monocyte-derived dendritic cells stimulated by lipopolysaccharide
Transplant. Proc.
41
698-699
2009
Homo sapiens
Manually annotated by BRENDA team
Sakurai, T.; Yoshiga, D.; Ariyoshi, W.; Okinaga, T.; Kiyomiya, H.; Furuta, J.; Yoshioka, I.; Tominaga, K.; Nishihara, T.
Essential role of mitogen-activated protein kinases in IL-17A-induced MMP-3 expression in human synovial sarcoma cells
BMC Res. Notes
9
68
2016
Homo sapiens, Homo sapiens (P27361)
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
Ma, B.; Wells, A.
The mitogen-activated protein (MAP) kinases p38 and extracellular signal-regulated kinase (ERK) are involved in hepatocyte-mediated phenotypic switching in prostate cancer cells
J. Biol. Chem.
289
11153-11161
2014
Homo sapiens
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
Bardwell, A.J.; Bardwell, L.
Two hydrophobic residues can determine the specificity of mitogen-activated protein kinase docking interactions
J. Biol. Chem.
290
26661-26674
2015
Homo sapiens (P45983), Homo sapiens (P45984), Homo sapiens (Q15759), Mus musculus (P63085)
Manually annotated by BRENDA team
Maisonneuve, P.; Caillet-Saguy, C.; Vaney, M.; Bibi-Zainab, E.; Sawyer, K.; Raynal, B.; Haouz, A.; Delepierre, M.; Lafon, M.; Cordier, F.; Wolff, N.
Molecular basis of the interaction of the human protein tyrosine phosphatase non-receptor type 4 (PTPN4) with the mitogen-activated protein kinase p38gamma
J. Biol. Chem.
291
16699-16708
2016
Homo sapiens (P53778), Homo sapiens
Manually annotated by BRENDA team
Choi, Y.H.; Yang, D.J.; Kulkarni, A.; Moh, S.H.; Kim, K.W.
Mycosporine-like amino acids promote wound healing through focal adhesion kinase (FAK) and mitogen-activated protein kinases (MAP kinases) signaling pathway in keratinocytes
Mar. Drugs
13
7055-7066
2015
Homo sapiens (P27361), Homo sapiens (P28482), Homo sapiens (P45983)
Manually annotated by BRENDA team
Naidu, S.; Sutherland, C.; Zhang, Y.; Risco, A.; de la Vega, L.; Caunt, C.; Hastie, C.; Lamont, D.; Torrente, L.; Chowdhry, S.; Benjamin, I.; Keyse, S.; Cuenda, A.; Dinkova-Kostovaa, A.
Heat shock factor 1 is a substrate for p38 mitogen-activated protein kinases
Mol. Cell. Biol.
36
2403-2417
2016
Homo sapiens
Manually annotated by BRENDA team
Qin, W.; Li, S.; Miao, Y.; Shi, Q.; Wang, Y.; Li, J.; Chen, Z.; Wang, J.; Ling, C.
Triptolide induces mitochondrial apoptosis through modulating dual specificity phosphatase 1/mitogen-activated protein kinases cascade in osteosarcoma cells
Neoplasma
65
21-33
2018
Homo sapiens
Manually annotated by BRENDA team