Information on EC 2.7.11.24 - mitogen-activated protein kinase and Organism(s) Homo sapiens and UniProt Accession Q15759

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EC Tree 2 Transferases 2.7 Transferring phosphorus-containing groups 2.7.11 Protein-serine/threonine kinases 2.7.11.24 mitogen-activated protein kinase

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.

The taxonomic range for the selected organisms is: Homo sapiens
The enzyme appears in selected viruses and cellular organisms

Reaction Schemes

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+

a [protein]-(L-serine/L-threonine)

=

+

a [protein]-(L-serine/L-threonine) phosphate

+

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

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MAPK

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MAPK11

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mitogen-activated protein kinase 11

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491002, 491716, 491718, 491789, 491790, 491791

p38-2

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p38beta

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491791, 740723, 740739

BMK1

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c-Jun N-terminal kinase

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c-jun N-terminal kinase 1

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c-Jun N-terminal kinase 2

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c-Jun N-terminal kinase 3

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c-Jun NH2-terminal kinase

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c-jun NH2-terminal MAPK

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cp38a

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-

-

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cp38b

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-

-

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CSAID binding protein

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-

-

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CSBP

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-

-

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Cytokine suppressive anti-inflammatory drug binding protein

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-

-

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ERK

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ERK1

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ERK1/2

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693505, 701309, 702513, 703019, 703255, 703561, 705322, 740720, 762008

ERK2

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ERK3

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ERK5

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-

-

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extracellular regulated kinase

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extracellular signal-regulated kinase

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extracellular signal-regulated kinase 1

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extracellular signal-regulated kinase 1/2

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extracellular signal-regulated kinase 2

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extracellular signal-regulated kinases-1/2

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extracellular signal-related kinase

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JNK

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JNK 2

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JNK/SAPK1c

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JNK1

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JNK1/2

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JNK1alpha1

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JNK2

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JNK2alpha2

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JNK3

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MAP kinase

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MAP kinase MXI2

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-

-

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MAP kinase p38 beta

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-

-

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MAP kinase p38 delta

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-

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MAP kinase p38 gamma

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-

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MAP kinase p38a

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-

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MAP kinase p38alpha

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-

-

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MAP kinase p38b

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-

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MAPK

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MAPK kinase

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MAPK12

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MAPK14

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MAPK3

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MAPK8

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MAPK9

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MEK

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MEK1/2

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mitogen-activated kinase

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mitogen-activated protein kinase

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mitogen-activated protein kinase 1

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mitogen-activated protein kinase 10

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mitogen-activated protein kinase 13

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491711, 491712, 491713, 491714, 491715, 491716, 491717, 491718

mitogen-activated protein kinase 3

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mitogen-activated protein kinase 4

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mitogen-activated protein kinase 6

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mitogen-activated protein kinase 7

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mitogen-activated protein kinase 8

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491760, 491761, 491762, 491763

mitogen-activated protein kinase 9

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491760, 491761, 491764, 491765

Mitogen-activated protein kinase p38 beta

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-

-

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Mitogen-activated protein kinase p38 delta

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-

-

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Mitogen-activated protein kinase p38 gamma

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Mitogen-activated protein kinase p38a

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Mitogen-activated protein kinase p38alpha

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Mitogen-activated protein kinase p38b

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-

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mitogen-activated protein kinase p44erk1

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mitogen-activated protein kinase/extracellular signal-regulated kinase 1/2 kinase

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p38

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p38 MAP kinase

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p38 MAPK

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p38 MAPKalpha

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p38 mitogen activated protein kinase

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p38 mitogen-activated protein kinase

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p38 mitogen-activated protein kinase alpha

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p38 protein

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p38-delta mitogen-activated protein kinase

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p38-MAPK

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p38alpha

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p38alpha MAP kinase

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p38alpha mitogen-activated protein kinase

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P38alpha-MAPKAP kinase 2

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p38b

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p38beta

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isoform

p38delta

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p38gamma

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p38MAPK

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p42

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p44

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p493F12 kinase

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p97MAPK

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SAPK

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SAPK2A

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-

-

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SAPK2a/p38

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SAPK2b/p38beta

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SAPK3/p38gamma

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SAPK4

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SAPK4/p38delta

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SAPKalphaI/JNK2

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signal-regulated kinase 3

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stress-activated protein kinase 2a

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-

-

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stress-activated protein kinase-4

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additional information

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the enzyme belongs to the MAPK superfamily of enzymes

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phospho group transfer

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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.

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142243-02-5

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ATP + Elk-1

ADP + phosphorylated Elk-1

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor
Products: -

?

ATP + MAPKAPK2

ADP + phosphorylated MAPKAPK2

show the reaction diagram

Substrates: -
Products: -

?

ATP + Net

ADP + phosphorylated Net

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor
Products: -

?

ATP + a protein

ADP + a phosphoprotein

show the reaction diagram

show

ATP + ATF-2

ADP + phosphorylated ATF-2

show the reaction diagram

show

ATP + ATF2

ADP + a phosphorylated ATF2

show the reaction diagram

Substrates: substrate in assay, biotinylated ATF2
Products: -

?

ATP + ATF2

ADP + phosphorylated ATF2

show the reaction diagram

show

ATP + Bcl-2

ADP + phosphorylated Bcl-2

show the reaction diagram

Substrates: -
Products: -

?

ATP + c-Jun

ADP + phosphorylated c-Jun

show the reaction diagram

show

ATP + c-Jun activation domain

ADP + phosphorylated c-Jun activation domain

show the reaction diagram

show

ATP + c-Jun transcription factor

ADP + phosphorylated c-Jun transcription factor

show the reaction diagram

-

Substrates: JNK phosphorylates the N-terminal transactivation domain of c-Jun transcription factor
Products: -

?

ATP + Elk-1

ADP + phosphorylated Elk-1

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor with modified D-site by swapping two hydrophobic residues
Products: -

?

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

-

Substrates: FITC-labeled ERK substrate peptide
Products: -

?

ATP + focal adhesion kinase

ADP + phosphorylated focal adhesion kinase

show the reaction diagram

P27361, P28482, P45983

Substrates: phosphorylation of FAK at S910, which promotes the disassembly of focal adhesion (hemidesmosome disruption) during cell migration
Products: -

?

ATP + GST-c-Jun

ADP + phosphorylated GST-c-Jun

show the reaction diagram

-

Substrates: substrate in kinase activity assay
Products: -

?

ATP + heat shock factor 1

ADP + phosphorylated heat shock factor 1

show the reaction diagram

-

Substrates: phosphorylation at Ser-326, Ser-303 and Ser-307, better substrate for p38gamma than for any of the other p38 isoforms
Products: -

?

ATP + human glucocorticoid receptor

ADP + phosphorylated human glucocorticoid receptor

show the reaction diagram

show

ATP + IRS-1

ADP + phosphorylated IRS-1

show the reaction diagram

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Substrates: phosphorylation of the insulin receptor substrate IRS-1 at serine 307
Products: -

?

ATP + Lin-1

ADP + phosphorylated Lin-1

show the reaction diagram

show

ATP + MAPK

ADP + phosphorylated MAPK

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + MAPKAP kinase-2

ADP + phosphorylated MAPKAP kinase-2

show the reaction diagram

Substrates: -
Products: -

?

ATP + MAPKAP kinase-3

ADP + phosphorylated MAPKAP kinase-3

show the reaction diagram

Substrates: -
Products: -

?

ATP + MAPKAPK2

ADP + phosphorylated MAPKAPK2

show the reaction diagram

Substrates: -
Products: -

?

ATP + MAPKAPK2-peptide

ADP + phosphorylated MAPKAPK2-peptide

show the reaction diagram

-

Substrates: the peptide substrate is derived from a sequence of a mitogen-activated protein kinase activated protein kinase-2, MAPKAPK2, phopshorylation site
Products: -

?

ATP + MK2

ADP + phosphorylated MK2

show the reaction diagram

-

Substrates: -
Products: -

?

ATP + MMP-9

ADP + phosphorylated MMP-9

show the reaction diagram

show

ATP + multifunctional protein CAD

ADP + phosphorylated multifunctional protein CAD

show the reaction diagram

show

ATP + myelin basic protein

ADP + phosphorylated myelin basic protein

show the reaction diagram

-

Substrates: substrate in in vitro kinase assay
Products: -

?

ATP + Net

ADP + phosphorylated Net

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor with modified D-site by swapping two hydrophobic residues
Products: -

?

ATP + protein

ADP + phosphoprotein

show the reaction diagram

show

ATP + protein APP

ADP + phosphorylated protein APP

show the reaction diagram

Substrates: -
Products: -

?

ATP + protein ATF2

ADP + phosphorylated protein ATF2

show the reaction diagram

show

ATP + protein EGFRP

ADP + phosphorylated protein EGFRP

show the reaction diagram

-

Substrates: epidermal growth factor receptor peptide, substrate in kinase activity assay
Products: -

?

ATP + transcription factor ATF2

ADP + phosphorylated transcription factor ATF2

show the reaction diagram

Substrates: -
Products: -

?

ATP + transcription factor Elk-1

ADP + phosphorylated transcription factor Elk-1

show the reaction diagram

Substrates: -
Products: -

?

ATP + transcription factor SAP-1

ADP + phosphorylated transcription factor SAP-1

show the reaction diagram

Substrates: -
Products: -

?

additional information

?

-

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Go to Natural Substrate Search

ATP + Elk-1

ADP + phosphorylated Elk-1

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor
Products: -

?

ATP + MAPKAPK2

ADP + phosphorylated MAPKAPK2

show the reaction diagram

Substrates: -
Products: -

?

ATP + Net

ADP + phosphorylated Net

show the reaction diagram

P45983, P45984, Q15759

Substrates: an ETS family transcription factor
Products: -

?

ATP + a protein

ADP + a phosphoprotein

show the reaction diagram

show

ATP + ATF2

ADP + phosphorylated ATF2

show the reaction diagram

P45983, P45984, Q15759

Substrates: -
Products: -

?

ATP + c-Jun

ADP + phosphorylated c-Jun

show the reaction diagram

show

ATP + human glucocorticoid receptor

ADP + phosphorylated human glucocorticoid receptor

show the reaction diagram

-

Substrates: 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
Products: -

?

ATP + Lin-1

ADP + phosphorylated Lin-1

show the reaction diagram

Substrates: substrate of ERK2, negative regulation of Lin-1
Products: -

?

ATP + MAPKAPK2

ADP + phosphorylated MAPKAPK2

show the reaction diagram

Substrates: -
Products: -

?

ATP + MMP-9

ADP + phosphorylated MMP-9

show the reaction diagram

-

Substrates: 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
Products: -

?

ATP + multifunctional protein CAD

ADP + phosphorylated multifunctional protein CAD

show the reaction diagram

-

Substrates: 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
Products: -

?

additional information

?

-

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ATP

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ATP

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Mg2+

P45983, P45984, Q15759

required

Ca2+

-

partially restores the ability of the protein to dimerize

Mg2+

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(1R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)cyclohexanol

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(1R,2S)-2-[([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)methyl]cyclohexanol

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(2R)-2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol

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(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

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RO4927350

(3-amino-1-oxido-2-phenylpyridin-4-yl)(phenyl)methanone

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(3R)-3-([4-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]pyrimidin-2-yl]amino)butanoic acid

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(R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide

show

(R)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2,3-dimethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-chlorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-ethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-hydroxyphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(2-trifluoromethylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-phenyl-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(3-fluoro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(4-chloro-2-fluorophenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(4-chloro-2-methylphenylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-4-[2-(benzo[d]1,3-dioxolylamino)-5-methylpyrimidin-4-yl]-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide

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(S)-N-(2-hydroxyl-1-phenylethyl)-4-[5-methyl-2-(phenylamino)-pyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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(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

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(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[-2-(2,3-dihydro-1H-inden-4-ylamino)-5-methylpyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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(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

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(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

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(S)-N-[1-(3-chlorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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(S)-N-[1-(3-fluorophenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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(S)-N-[1-(3-methylphenyl)-2-hydroxyethyl]-4-[5-methyl-2-(phenylamino)pyrimidin-4-yl]-1H-pyrrole-2-carboxamide

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1-((S)-4-(6-(3-(cyclopropylamino)-6-methylbenzo[d]isoxazol-7-yl)phthalazin-1-yl)-3-methylpiperazin-1-yl)ethanone

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1-(2,6-dichloro-phenyl)-1-(4-(4-fluorophenyl)thiazol-2-yl)urea

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1-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol

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1-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-2-ol

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1-methyl-2-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-benzimidazole

-

-

2,2'-disulfanediylbis(1,3-benzothiazole)

-

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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

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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

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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

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2-([4-[4-(4-fluorophenyl)-1-(2-methoxyethyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol

-

2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)-3-methylbutan-1-ol

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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)butan-1-ol

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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)ethanol

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2-([4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridin-2-yl]amino)propan-1-ol

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2-bromo-N-[3-chloro-2-(4-prop-2-en-1-ylpiperazin-1-yl)phenyl]-1,3-thiazole-5-carboxamide

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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

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2-fluoro-4-[2-(methylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine

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2-fluoro-4-[2-(phenylsulfanyl)-4-[3-(trifluoromethyl)phenyl]-1H-imidazol-5-yl]pyridine

-

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

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2-[(1,5-dimethylhexyl)oxy]-4-[4-(4-fluorophenyl)-2-(methylsulfanyl)-1H-imidazol-5-yl]pyridine

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2-[(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-(3-phenoxyphenoxy)phenyl]propanoyl-CoA

-

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

show

BIRB-796

show

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

L-790070

-

MKK4

show

-

MKK4 mutant F48K

P45983, P45984, Q15759

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

show

-

ML3375

-

ML3403

-

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

PD169316

-

PD98059

show

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

RWJ67657

-

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

show

SB203580

show

SB203580-iodo

-

SB203580-sulfone

-

SB220025

-

SB239063

-

SB242235

show

SC68376

-

SCIO-469

-

SKF86002

-

SP600125

show

SR3451

-

-

SR3576

-

-

SR3582

-

-

SR3583

-

-

SR4018

-

-

SR4276

-

-

SR4326

-

-

SR4642

-

-

SR4643

-

-

TAK-715

-

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

show

VX-702

-

[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

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[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-(2-methylphenyl)-1-oxidopyridin-4-yl](phenyl)methanone

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[3-amino-2-(3-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-(4-chloro-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-(4-chlorophenyl)-1-oxidopyridin-4-yl](phenyl)methanone

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[3-amino-2-(4-hydroxy-2-methylphenyl)-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-[2-methyl-4-(2-morpholin-4-ylethoxy)phenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[3-amino-2-[4-(2-methoxyethoxy)-2-methylphenyl]-1-oxidopyridin-4-yl](2,4-difluorophenyl)methanone

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[Nle4, D-Phe7]alpha-melanocyte stimulating hormone

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NDP-MSH, the melanocortin agonist dose-dependently inhibits JNK activity in HEK-293 cells stably expressing the human melanocortin receptor type 4

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amitriptyline

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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

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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

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glucocorticoids

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activate p38 MAPK, e.g. by induction of activating MKK3

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interleukin-1beta

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activates the MAPKs, dexamethasone inhibits this activation

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interleukin-I

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lipopolysaccharide

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mitogen-activated protein kinase kinase 6

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MKK6

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MKK3

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MKK6

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mycosporine-glycine

P27361, P28482, P45983

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

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the enzyme is activated by exposure to 0.02 mM phenethyl isothiocyanate

porphyra

P27361, P28482, P45983

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

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purvalanol

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17% activation of SAPK2b/p38beta

Ras

Ras induces phosphorylation of c-Jun by JNKs

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shinorine

P27361, P28482, P45983

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

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thapsigargin

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stimulates 4-5fold the expression of p44/p42

TNF-alpha

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transforming growth factor-beta

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i.e. TGF-beta, activates p38, butenoside inhibits this activation

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tumor necrosis factor-alpha

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additional information

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