| + |
BRAF | up-regulates 
phosphorylation
|
MAP2K2 |
0.739 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-42664 |
Ser222 |
VSGQLIDsMANSFVG |
Homo sapiens |
|
| pmid |
sentence |
| 8668348 |
We show that, consequently, b-raf interacts with mek-1 and mek-2 with a better affinity than does c-raf-1, thus strengthening the notion that b-raf is a stronger mek activator than c-raf-l. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-42668 |
Ser226 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 8668348 |
We show that, consequently, b-raf interacts with mek-1 and mek-2 with a better affinity than does c-raf-1, thus strengthening the notion that b-raf is a stronger mek activator than c-raf-l. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| Tissue: |
Brain |
| + |
RAF1 | up-regulates
phosphorylation
|
MAP2K2 |
0.72 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-262292 |
Ser222 |
VSGQLIDsMANSFVG |
Homo sapiens |
|
| pmid |
sentence |
| 8157000 |
To understand the mechanism of activation of MAPKK, we have identified Ser217 and Ser221 of MAPKK1 as the sites phosphorylated by p74raf-1. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-36553 |
Ser226 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 8157000 |
To understand the mechanism of activation of MAPKK, we have identified Ser217 and Ser221 of MAPKK1 as the sites phosphorylated by p74raf-1. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
MAP3K8 | up-regulates
phosphorylation
|
MAP2K2 |
0.415 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-129694 |
Ser222 |
VSGQLIDsMANSFVG |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 15466476 |
Cot proteins were used in an in vitro kinase assay using mek as a substrate. Samples were analyzed by western blotting. As seen in the cascade activity assay only wild-type cot was active against mekregulation of cot is of great interest to the signaling field since the cot/mek/erk pathway potentially plays a role in the etiology of inflammatory autoimmune diseases. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-129698 |
Ser226 |
LIDSMANsFVGTRSY |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 15466476 |
Cot proteins were used in an in vitro kinase assay using mek as a substrate. Samples were analyzed by western blotting. As seen in the cascade activity assay only wild-type cot was active against mekregulation of cot is of great interest to the signaling field since the cot/mek/erk pathway potentially plays a role in the etiology of inflammatory autoimmune diseases. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
PDPK1 | up-regulates
phosphorylation
|
MAP2K2 |
0.259 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-125176 |
Ser226 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 15175348 |
The identified pdk1 phosphorylation sites in mek1 and mek2 are ser222 and ser226, respectively, and are known to be essential for full activation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K2 | down-regulates activity 
phosphorylation
|
CASP9 |
0.354 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-249386 |
Thr125 |
PEVLRPEtPRPVDIG |
|
|
| pmid |
sentence |
| 12792650 |
Inhibition of caspase-9 through phosphorylation at Thr 125 by ERK MAPK|The opposing protein kinase activity is overcome by treatment with the broad-specificity kinase inhibitor staurosporine or with inhibitors of MEK1/2 |
|
| Publications: |
1 |
| + |
MAP2K2 | up-regulates
phosphorylation
|
MAPK1 |
0.733 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-86709 |
Thr185 |
HDHTGFLtEYVATRW |
Homo sapiens |
|
| pmid |
sentence |
| 11971971 |
Mapk1 is phosphorylated by map2k1/mek1 and map2k2/mek2 on thr-185 and tyr-187 in response to external stimuli like insulin or ngf. Both phosphorylations are required for activity. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-86713 |
Tyr187 |
HTGFLTEyVATRWYR |
Homo sapiens |
|
| pmid |
sentence |
| 11971971 |
Mapk1 is phosphorylated by map2k1/mek1 and map2k2/mek2 on thr-185 and tyr-187 in response to external stimuli like insulin or ngf. Both phosphorylations are required for activity. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
MAP2K2 | up-regulates
phosphorylation
|
MAPK3 |
0.73 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-19240 |
Thr202 |
HDHTGFLtEYVATRW |
Homo sapiens |
|
| pmid |
sentence |
| 1411546 |
The primary structure of mek, a protein kinase that phosphorylates the erk gene product |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-19244 |
Tyr204 |
HTGFLTEyVATRWYR |
Homo sapiens |
|
| pmid |
sentence |
| 1411546 |
The primary structure of mek, a protein kinase that phosphorylates the erk gene product |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| Tissue: |
Brain |
| + |
MAP2K2 | up-regulates activity
phosphorylation
|
MAPK1 |
0.733 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258996 |
|
|
Mus musculus |
|
| pmid |
sentence |
| 11730323 |
Raf proteins have been shown to phosphorylate and activate MAPKKs (MAP kinase kinases) called MEKs (MAPK or ERK kinases) which in turn phosphorylate and activate MAPKs (MAP kinases) called ERKs |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189933 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K2 | up-regulates
binding
|
PPARG |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-179393 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18596912 |
The genomic activity of ppargamma is modulated, in addition to ligand binding, by phosphorylation of a serine residue by mapks, such as extracellular signal-regulated protein kinases-1/2 (erk-1/2), or by nucleocytoplasmic compartmentalization through the erk activators mapk kinases-1/2 (mek-1/2). These mapks phosphorylate (in humans) ser 84 in the ppargamma1 and ser 114 in ppargamma2 isoform. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K2 | up-regulates
phosphorylation
|
ERK1/2 |
0.735 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244637 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11971971 |
Mapk1 is phosphorylated by map2k1/mek1 and map2k2/mek2 on thr-185 and tyr-187 in response to external stimuli like insulin or ngf. Both phosphorylations are required for activity. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
trametinib | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-192826 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PD318088 | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205740 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
U0126 | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-104942 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11160424 |
The mek1/2 inhibitors pd98059, sl327, and u0126 have been extensively used to implicate erk1/2 in neuroplasticity. U0126 was found to functionally antagonize ap-1 transcriptional activity via noncompetitive the dual specificity kinase mek with an ic50 of 0.07 microm for mek 1 and 0.06 microm for mek 2. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-62895 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 9873633 |
The mek1/2 inhibitors pd98059, sl327, and u0126 have been extensively used to implicate erk1/2 in neuroplasticity. U0126 was found to functionally antagonize ap-1 transcriptional activity via noncompetitive the dual specificity kinase mek with an ic50 of 0.07 microm for mek 1 and 0.06 microm for mek 2. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
SL-327 | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-104930 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11160424 |
The mek1/2 inhibitors pd98059, sl327, and u0126 have been extensively used to implicate erk1/2 in neuroplasticity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide | down-regulates activity
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258204 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
MAP2K2 | up-regulates activity
phosphorylation
|
ERK1/2 |
0.735 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258995 |
|
|
Mus musculus |
|
| pmid |
sentence |
| 11730323 |
Raf proteins have been shown to phosphorylate and activate MAPKKs (MAP kinase kinases) called MEKs (MAPK or ERK kinases) which in turn phosphorylate and activate MAPKs (MAP kinases) called ERKs |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
MAP2K2 | up-regulates activity
phosphorylation
|
MAPK3 |
0.73 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258997 |
|
|
Mus musculus |
|
| pmid |
sentence |
| 11730323 |
Raf proteins have been shown to phosphorylate and activate MAPKKs (MAP kinase kinases) called MEKs (MAPK or ERK kinases) which in turn phosphorylate and activate MAPKs (MAP kinases) called ERKs |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
2-(2-amino-3-methoxyphenyl)chromen-4-one | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-104921 |
|
|
Homo sapiens |
Neuron |
| pmid |
sentence |
| 11160424 |
The mek1/2 inhibitors pd98059, sl327, and u0126 have been extensively used to implicate erk1/2 in neuroplasticity. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205746 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| Tissue: |
Brain |
| + |
PPP2CA | down-regulates
dephosphorylation
|
MAP2K2 |
0.47 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-166652 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 20626350 |
In particular, p38 mapk activity stimulates the physical association between ppa2 and mkk1/2- erk1/2 complex, leading to mkk1/2 dephosphorilation by pp2a. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191024 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ARAF | up-regulates
phosphorylation
|
MAP2K2 |
0.742 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-175142 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 21779497 |
Active raf phosphorylates mek. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
selumetinib | down-regulates activity
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258281 |
|
|
in vitro |
|
| pmid |
sentence |
| 22037378 |
Our data set represents the most detailed comprehensive assessment of the reactivity of known and clinical kinase inhibitors across the kinome published to date. | The data also show that for at least 15 of the 27 kinases that are the primary, intended targets for the compounds tested and that are represented in the assay panel, selective inhibitors, as assessed by both absolute selectivity across the kinome and selectivity relative to the primary target, are among the 72 tested here. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
trametinib | down-regulates activity
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259448 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 26347206 |
Trametinib (Mekinist™) is a reversible and highly selective allosteric inhibitor of MEK1 and MEK2 with anticancer activity against metastatic melanoma carrying the BRAF V600 mutation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K2 | up-regulates
phosphorylation
|
Gbeta |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-269895 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 1411546 |
The primary structure of mek, a protein kinase that phosphorylates the erk gene product |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Brain |
| + |
U0126.EtOH | down-regulates
chemical inhibition
|
MAP2K2 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-207606 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
MAP2K2
- 
- 