| + |
MAP2K1 | up-regulates quantity by stabilization 
phosphorylation
|
TET2 |
0.249 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277891 |
Ser1107 |
VLNNFIEsPSKLLDT |
Homo sapiens |
HCC-827 Cell |
| pmid |
sentence |
| 38461173 |
TET2 was stabilized by MEK1 phosphorylation at Ser 1107, while MEK1 inactivation promoted its proteasome degradation by enhancing the recruitment of CUL7FBXW11. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K1 | down-regulates 
phosphorylation
|
TAL1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-116149 |
Ser122 |
DGRMVQLsPPALAAP |
Homo sapiens |
|
| pmid |
sentence |
| 11904294 |
We found that hypoxia greatly accelerated tal1 turnover in these cells through mitogen-activated protein kinase (mapk)2-mediated phosphorylation, ubiquitination, and proteasomal degradation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ARAF | up-regulates
phosphorylation
|
MAP2K1 |
0.73 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236451 |
Ser218 |
VSGQLIDsMANSFVG |
Homo sapiens |
HeLa Cell |
| pmid |
sentence |
| 8621729 |
Our data demonstrated that a-raf is, indeed, a mek1 activator and may play a role in growth factor signaling|The immunoprecipitates were assayed for GST-MEK1 activation. D, activation of MEK1 by A-Raf requires the presence of serine residue 218 and 222. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235944 |
Ser222 |
LIDSMANsFVGTRSY |
Homo sapiens |
HeLa Cell |
| pmid |
sentence |
| 8621729 |
Our data demonstrated that a-raf is, indeed, a mek1 activator and may play a role in growth factor signaling|The immunoprecipitates were assayed for GST-MEK1 activation. D, activation of MEK1 by A-Raf requires the presence of serine residue 218 and 222. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
MAP3K1 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.647 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235587 |
Ser218 |
VSGQLIDsMANSFVG |
Mus musculus |
NIH-3T3 Cell |
| pmid |
sentence |
| 8131746 |
Phosphorylation at ser-218 and ser-222 by map kinase kinase kinases (raf or mekk1) positively regulates mek1 kinase activity. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235564 |
Ser222 |
LIDSMANsFVGTRSY |
Mus musculus |
NIH-3T3 Cell |
| pmid |
sentence |
| 8131746 |
Phosphorylation at ser-218 and ser-222 by map kinase kinase kinases (raf or mekk1) positively regulates mek1 kinase activity. |
|
| Publications: |
2 |
Organism: |
Mus Musculus |
| + |
MAP3K8 | up-regulates
phosphorylation
|
MAP2K1 |
0.557 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-129690 |
Ser218 |
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-36449 |
Ser222 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 8131746 |
Activation of mek family kinases requires phosphorylation of two conserved ser/thr residues.Phosphopeptide analysis demonstrated that serine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-36453 |
Ser244 |
GTHYSVQsDIWSMGL |
Homo sapiens |
|
| pmid |
sentence |
| 8131746 |
Activation of mek family kinases requires phosphorylation of two conserved ser/thr residues.Phosphopeptide analysis demonstrated that serine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-36457 |
Ser248 |
SVQSDIWsMGLSLVE |
Homo sapiens |
|
| pmid |
sentence |
| 8131746 |
Activation of mek family kinases requires phosphorylation of two conserved ser/thr residues.Phosphopeptide analysis demonstrated that serine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf |
|
| Publications: |
4 |
Organism: |
Homo Sapiens |
| + |
BRAF | up-regulates activity
phosphorylation
|
MAP2K1 |
0.781 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235475 |
Ser218 |
VSGQLIDsMANSFVG |
Mus musculus |
NIH-3T3 Cell |
| pmid |
sentence |
| 8131746 |
Activation of mek family kinases requires phosphorylation of two conserved ser/thr residueserine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-39054 |
Ser222 |
LIDSMANsFVGTRSY |
in vitro |
|
| pmid |
sentence |
| 8413257 |
Raf-1 phosphorylation of MEK activated it, as judged by its ability to stimulate the phosphorylation of myelin basic protein by glutathione S-transferase-ERK1. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-39058 |
Ser248 |
SVQSDIWsMGLSLVE |
in vitro |
|
| pmid |
sentence |
| 8413257 |
Raf-1 phosphorylation of MEK activated it, as judged by its ability to stimulate the phosphorylation of myelin basic protein by glutathione S-transferase-ERK1. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-39062 |
Ser252 |
DIWSMGLsLVEMAVG |
in vitro |
|
| pmid |
sentence |
| 8413257 |
Raf-1 phosphorylation of MEK activated it, as judged by its ability to stimulate the phosphorylation of myelin basic protein by glutathione S-transferase-ERK1. |
|
| Publications: |
4 |
Organism: |
Mus Musculus, In Vitro |
| + |
MAP3K21 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-260767 |
Ser218 |
VSGQLIDsMANSFVG |
Homo sapiens |
|
| pmid |
sentence |
| 23319808 |
These experiments showed that MEK1 is phosphorylated by MLK4 on Ser217/221 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-260768 |
Ser222 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 23319808 |
These experiments showed that MEK1 is phosphorylated by MLK4 on Ser217/221 |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
RAF1 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.739 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235987 |
Ser218 |
VSGQLIDsMANSFVG |
Homo sapiens |
|
| pmid |
sentence |
| 10359597 |
Among other effectors, active ras binds and activates the raf kinase, iniziating a kinase cascade involving serine phosporylation of mek1/2 (mapkk) and tyrosine and threonine phosphorylation of erk1/2 active raf phosphorylates mek phospholpeptide analysis demostrated that serine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235991 |
Ser222 |
LIDSMANsFVGTRSY |
Homo sapiens |
|
| pmid |
sentence |
| 10359597 |
Among other effectors, active ras binds and activates the raf kinase, iniziating a kinase cascade involving serine phosporylation of mek1/2 (mapkk) and tyrosine and threonine phosphorylation of erk1/2 ras activation leads to raf and subsequently mek activation. Phospholipide analysis demostrated that serine residues 218 and 222 of human mek1 are the primary sites for phosphorylation by c-raf. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| Tissue: |
Ovary |
| + |
PDPK1 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.273 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236633 |
Ser222 |
LIDSMANsFVGTRSY |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 15175348 |
In vitro kinase assay revealed that the direct targets of pdk1 in the mapk pathway were the upstream mapk kinases mek1 and mek2. 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 |
| + |
MOS | up-regulates activity
phosphorylation
|
MAP2K1 |
0.468 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-260920 |
Ser222 |
LIDSMANsFVGTRSY |
Mus musculus |
|
| pmid |
sentence |
| 7731726 |
Our data indicate that Mos activated MEK1 in vitro as well as in vivo by phosphorylating Ser 222. |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
PAK1 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.564 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236002 |
Ser298 |
RTPGRPLsSYGMDSR |
Homo sapiens |
REF-52 Cell |
| pmid |
sentence |
| 12876277 |
We find that adhesion to fibronectin induces pak1-dependent phosphorylation of mek1 on s298 and that this phosphorylation is necessary for efficient activation of mek1 and subsequent mapk activation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PAK | up-regulates
phosphorylation
|
MAP2K1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-140039 |
Ser298 |
RTPGRPLsSYGMDSR |
Homo sapiens |
HeLa Cell |
| pmid |
sentence |
| 16129686 |
Inhibition of pak kinase activity dramatically decreased phosphorylation of mek1 at ser(298) in response to either pdgf or egf. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
MAP2K1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-251415 |
Ser304 |
LSSYGMDsRPPMAIF |
in vitro |
|
| pmid |
sentence |
| 8226933 |
MEK1 and MEK2 can also be activated by autophosphorylation. Tyrosine 304 may be a candidate for the autophosphorylation site in MEK1. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
MAP2K1 | down-regulates
phosphorylation
|
IRS1 |
0.358 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236611 |
Ser307 |
TRRSRTEsITATSPA |
Homo sapiens |
|
| pmid |
sentence |
| 11160134 |
Thus, at least three kinases mediate phosphorylation of ser307, including jnk, serine kinases in the pi 3-kinase cascade that are activated byinsulinor igf-1, and mek1-sensitive kinase cascades during tnf-alfa stimulation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Muscle |
| + |
MAP2K1 | down-regulates activity
phosphorylation
|
CASP9 |
0.45 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-249385 |
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 |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
MAPK1 |
0.741 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236447 |
Thr185 |
HDHTGFLtEYVATRW |
Homo sapiens |
BJ Cell |
| 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-235937 |
Tyr187 |
HTGFLTEyVATRWYR |
Homo sapiens |
BJ Cell |
| 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-258993 |
|
|
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 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235940 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 12270934 |
Mek1 as indicated by extensive phosphorylation of erk1 and erk2 during the initial 2 h of adipogenesis. |
|
| Publications: |
4 |
Organism: |
Homo Sapiens, Mus Musculus |
| + |
MAP2K1 | up-regulates
phosphorylation
|
MAPK3 |
0.743 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-59153 |
Thr202 |
HDHTGFLtEYVATRW |
Homo sapiens |
|
| pmid |
sentence |
| 9677429 |
The mek1 proline-rich insert is required for efficient activation of the mitogen-activated protein kinases erk1 and erk2 in mammalian cells. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-59157 |
Tyr204 |
HTGFLTEyVATRWYR |
Homo sapiens |
|
| pmid |
sentence |
| 9677429 |
The mek1 proline-rich insert is required for efficient activation of the mitogen-activated protein kinases erk1 and erk2 in mammalian cells. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-210176 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 12270934 |
Mek1 as indicated by extensive phosphorylation of erk1 and erk2 during the initial 2 h of adipogenesis. |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
CDK5/CDK5R1 | down-regulates activity
phosphorylation
|
MAP2K1 |
0.479 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-250653 |
Thr286 |
VEGDAAEtPPRPRTP |
Mus musculus |
NIH-3T3 Cell |
| pmid |
sentence |
| 11684694 |
Phosphorylation of MEK1 by cdk5/p35 down-regulates the mitogen-activated protein kinase pathway. | suggesting that Thr286 in MEK1 is a site of cdk5/p35 phosphorylation that inhibits MEK1 activity. |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
CDK1 | down-regulates
phosphorylation
|
MAP2K1 |
0.474 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-36112 |
Thr286 |
VEGDAAEtPPRPRTP |
Homo sapiens |
|
| pmid |
sentence |
| 8114697 |
P34cdc2 catalyzes the in vitro phosphorylation of mkk1 on both of these threonine residues and inactivates mkk1 enzymatic activity. Both sites are phosphorylated in vivo as well |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-36116 |
Thr292 |
ETPPRPRtPGRPLSS |
Homo sapiens |
|
| pmid |
sentence |
| 8114697 |
P34cdc2 catalyzes the in vitro phosphorylation of mkk1 on both of these threonine residues and inactivates mkk1 enzymatic activity. Both sites are phosphorylated in vivo as well |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
MAPK1 | down-regulates activity
phosphorylation
|
MAP2K1 |
0.741 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236335 |
Thr292 |
ETPPRPRtPGRPLSS |
Chlorocebus aethiops |
COS Cell |
| pmid |
sentence |
| 14993270 |
We propose that activation of erk during adhesion creates a feedback system in which erk phosphorylates mek1 on t292, and this in turn blocks additional s298 phosphorylation in response to integrin signaling. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236498 |
Thr386 |
IGLNQPStPTHAAGV |
Homo sapiens |
|
| pmid |
sentence |
| 10567369 |
An ERK2-binding site at the N terminus of MEK1 was reported to mediate their stable association. We examined the importance of this binding site in the feedback phosphorylation of mek1 on thr(292) and thr(386) by erk2 |
|
| Publications: |
2 |
Organism: |
Chlorocebus Aethiops, Homo Sapiens |
| + |
ERK1/2 | down-regulates activity
phosphorylation
|
MAP2K1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244557 |
Thr292 |
ETPPRPRtPGRPLSS |
Chlorocebus aethiops |
COS Cell |
| pmid |
sentence |
| 14993270 |
We propose that activation of erk during adhesion creates a feedback system in which erk phosphorylates mek1 on t292, and this in turn blocks additional s298 phosphorylation in response to integrin signaling. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244561 |
Thr386 |
IGLNQPStPTHAAGV |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 10567369 |
An ERK2-binding site at the N terminus of MEK1 was reported to mediate their stable association. We examined the importance of this binding site in the feedback phosphorylation of mek1 on thr(292) and thr(386) by erk2 |
|
| Publications: |
2 |
Organism: |
Chlorocebus Aethiops, Homo Sapiens |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
ARRB2 |
0.57 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-252027 |
Thr382 |
EFDTNYAtDDDIVFE |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 28169830 |
Here, we show that activation of serotonin 5-HT2C receptors, which engage Erk1/2 pathway via a _-arrestin-dependent mechanism, promotes MEK-dependent _-arrestin2 phosphorylation at Thr383 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
GSK3B |
0.349 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236622 |
Tyr216 |
RGEPNVSyICSRYYR |
Homo sapiens |
|
| pmid |
sentence |
| 15020233 |
In vitro kinase assay was carried out using a recombinant human active mek1 and we found that gsk-3beta was phosphorylated on tyr(216) by this kinase in a dose- and time-dependent manner. Further, the pretreatment of fibroblasts with u0126 inhibited serum-induced nuclear translocation of gsk-3beta. These results suggested that mek1/2 induces tyrosine phosphorylation of gsk-3beta and this cellular event might induce nuclear translocation of gsk-3beta. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Skin |
| + |
MAP2K1 | up-regulates
phosphorylation
|
Gbeta |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-269909 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 12270934 |
Mek1 as indicated by extensive phosphorylation of erk1 and erk2 during the initial 2 h of adipogenesis. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
MAPK3 |
0.743 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258994 |
|
|
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-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191021 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP2K1 | down-regulates 
|
MAPK14 |
0.661 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-178636 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18481201 |
Pd98059, a specific inhibitor of mek in addition, immunoblot and immunostaining analysis revealed that phosphorylation of erk was increased by treatment with sb203580;whereas pd98059 increased the phosphorylation of p38, which implies a seesaw-like balance between erk and p38 phosphorylation. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
trametinib | down-regulates activity
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259447 |
|
|
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 |
| + |
2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide | down-regulates activity
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258203 |
|
|
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 |
| + |
MAP2K1 | up-regulates activity
phosphorylation
|
ERK1/2 |
0.743 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235352 |
|
|
Mus musculus |
3T3-L1 Cell |
| pmid |
sentence |
| 12270934 |
MEK1 as indicated by extensive phosphorylation of ERK1 and ERK2 during the initial 2 h of adipogenesis. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258992 |
|
|
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: |
2 |
Organism: |
Mus Musculus |
| + |
selumetinib | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190191 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
U0126.EtOH | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-207603 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAP3K2 | up-regulates
phosphorylation
|
MAP2K1 |
0.424 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-107692 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11343802 |
Both mekk2 and mekk3 are able to activate the jun kinase pathway in vivo. However, following routine immunoprecipitation in triton x-100, mekk2 but not mekk3 is able to effectively phosphorylate both sek-1 and mek-1 and to undergo autophosphorylation |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
trametinib | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-192823 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
LAMTOR3 | up-regulates
binding
|
MAP2K1 |
0.599 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-130924 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15547943 |
We analyzed the ability of mp1 to bind to mek1, erk1, and to itself, and the regulation of these interactions. Gel filtration of cell lysates revealed two major mp1 peaks: a broad high molecular weight peak and a 28 kda complex. An mp1 mutant that lost mek1 binding no longer enhanced rasv12-stimulated erk1 activity, and functioned as a dominant negative, consistent with the concept that mp1 function depends on facilitating these oligomerizations. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
U0126 | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-104939 |
|
|
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-62892 |
|
|
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 |
| + |
FGFR1 | up-regulates 
|
MAP2K1 |
0.315 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-218010 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 12270934 |
Fibroblast growth factor-2 (FGF-2), in the presence of dexamethasone, isobutylmethylxanthine, and insulin, induces a prolonged activation of the MEK/ERK signaling pathway, which lasts for at least 12 h post-induction, and this activity is less sensitive to the MEK inhibitors |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
2-(2-amino-3-methoxyphenyl)chromen-4-one | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205743 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
WDR83 | up-regulates
binding
|
MAP2K1 |
0.506 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-124470 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 15118098 |
Morg1 specifically associates with several components of the erk pathway, including mp1, raf-1, mek, and erk, and stabilizes their assembly into an oligomeric complex. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR2 | up-regulates
|
MAP2K1 |
0.306 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235337 |
|
|
Mus musculus |
3T3-L1 Cell |
| pmid |
sentence |
| 12270934 |
Fibroblast growth factor-2 (FGF-2), in the presence of dexamethasone, isobutylmethylxanthine, and insulin, induces a prolonged activation of the MEK/ERK signaling pathway, which lasts for at least 12 h post-induction, and this activity is less sensitive to the MEK inhibitors |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
PPP2CA | down-regulates
dephosphorylation
|
MAP2K1 |
0.541 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-166649 |
|
|
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 |
| + |
selumetinib | down-regulates activity
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258280 |
|
|
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 |
| + |
MAP2K1 | up-regulates quantity by expression
transcriptional regulation
|
CEBPA |
0.265 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235325 |
|
|
Mus musculus |
3T3-L1 Cell |
| pmid |
sentence |
| 12270934 |
We further show that activation of mek1 significantly enhances the transactivation of the c/ebpalpha minimal promoter during the early phase of the differentiation process. |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
GIT1 | up-regulates activity
binding
|
MAP2K1 |
0.399 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-261245 |
|
|
Homo sapiens |
Hep-G2 Cell |
| pmid |
sentence |
| 23325602 |
We found both MAT2B variants interact with GIT1. MAT2B directly promoted binding of GIT1 and ERK2 to MEK1. MAT2B and GIT1 interact and are overexpressed in most human liver and colon cancer specimens. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-189930 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PD318088 | down-regulates
chemical inhibition
|
MAP2K1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205737 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
3.0
MAP2K1
- 
- 