| + |
MAPK3 | down-regulates 
phosphorylation
|
FGFR1 |
0.326 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-200884 |
Ser777 |
SMPLDQYsPSFPDTR |
Homo sapiens |
|
| pmid |
sentence |
| 23405013 |
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAPK14 | down-regulates
phosphorylation
|
FGFR1 |
0.278 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-166598 |
Ser777 |
SMPLDQYsPSFPDTR |
Homo sapiens |
|
| pmid |
sentence |
| 20626350 |
Fgfr1 translocation requires p38 mapk activation which phosphorylates the c-term tail of fgfr1 on ser777 |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
MAPK1 | down-regulates
phosphorylation
|
FGFR1 |
0.315 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-200880 |
Ser777 |
SMPLDQYsPSFPDTR |
Homo sapiens |
|
| pmid |
sentence |
| 23405013 |
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
ERK1/2 | down-regulates
phosphorylation
|
FGFR1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244541 |
Ser777 |
SMPLDQYsPSFPDTR |
Homo sapiens |
|
| pmid |
sentence |
| 23405013 |
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Luminal Breast Cancer |
| + |
PRKCE | up-regulates 
phosphorylation
|
FGFR1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-201671 |
Ser779 |
PLDQYSPsFPDTRSS |
Homo sapiens |
Neuron |
| pmid |
sentence |
| 23564461 |
Phosphorylation of serine 779 in fibroblast growth factor receptor 1 and 2 by protein kinase c(epsilon) regulates ras/mitogen-activated protein kinase signaling and neuronal differentiationour findings show that in addition to fgfr tyrosine phosphorylation, the phosphorylation of a conserved serine residue, ser(779), can quantitatively control ras/mapk signaling to promote specific cellular responses. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
RPS6KA3 | down-regulates quantity
phosphorylation
|
FGFR1 |
0.363 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276599 |
Ser789 |
DTRSSTCsSGEDSVF |
Homo sapiens |
U2-OS Cell |
| pmid |
sentence |
| 24141780 |
Both in vitro and in vivo experiments confirmed the interaction and we show that phosphorylated RSK2 binds to and phosphorylates serine 789 in the C-terminal tail of FGFR1.prevention of FGFR1 phosphorylation by inhibition of RSK2 activity or mutation of serine 789 to alanine reduced FGFR1 endocytosis and ubiquitination explaining mechanistically the prolonged signaling activity. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates
phosphorylation
|
LDHA |
0.376 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-176730 |
Tyr10 |
TLKDQLIyNLLKEEQ |
Homo sapiens |
|
| pmid |
sentence |
| 21969607 |
We found that the oncogenic receptor tyrosine kinase fgfr1 directly phosphorylates ldh-a. Phosphorylation at y10 and y83 enhances ldh-a activity by enhancing the formation of active, tetrameric ldh-a and the binding of ldh-a substrate nadh, respectively. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-176734 |
Tyr83 |
KIVSGKDyNVTANSK |
Homo sapiens |
|
| pmid |
sentence |
| 21969607 |
We found that the oncogenic receptor tyrosine kinase fgfr1 directly phosphorylates ldh-a. Phosphorylation at y10 and y83 enhances ldh-a activity by enhancing the formation of active, tetrameric ldh-a and the binding of ldh-a substrate nadh, respectively. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates activity
phosphorylation
|
AMOTL2 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-271869 |
Tyr107 |
KGEELPTyEEAKAHS |
Homo sapiens |
HEK-293 Cell |
| pmid |
sentence |
| 21937427 |
These data support an idea that Amotl2 Tyr-103 can be phosphorylated by FGF receptor tyrosine kinase activity. We then determined whether Amotl2 Tyr-103 is required for its interaction with c-Src. |Amotl2 promotes MAPK/ERK activation via c-Src, which is dependent on phosphorylation of tyrosine residue at position 103 but independent of the C-terminal PDZ-binding domain. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates
phosphorylation
|
BCAR1 |
0.259 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-82760 |
Tyr128 |
SKAQQGLyQVPGPSP |
Homo sapiens |
|
| pmid |
sentence |
| 11019781 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98488 |
Tyr128 |
SKAQQGLyQVPGPSP |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98492 |
Tyr249 |
APGPQDIyDVPPVRG |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98496 |
Tyr306 |
PSNHHAVyDVPPSVS |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98500 |
Tyr327 |
PLLREETyDVPPAFA |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98569 |
Tyr410 |
GVVDSGVyAVPPPAE |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Five tyrosine phosphorylation sites were identified in p130cas on tyr-128, tyr-249, tyr-306, tyr-327, and tyr-410. These tyrosine residues are all located in the substrate domain of p130cas that mediates binding to the sh2 domain of the adaptor molecule crk. Fgf-1-transduced fibroblasts demonstrated a > 10-fold increase in migration, an observation correlated with increased tyrosine phosphorylation of p125fak and p130cas. |
|
| Publications: |
6 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates
phosphorylation
|
PDK1 |
0.355 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191719 |
Tyr136 |
AEDAKAIyDFTDTVI |
Homo sapiens |
|
| pmid |
sentence |
| 22195962 |
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-191723 |
Tyr243 |
ARRLCDLyYINSPEL |
Homo sapiens |
|
| pmid |
sentence |
| 22195962 |
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-193454 |
Tyr244 |
RRLCDLYyINSPELE |
Homo sapiens |
|
| pmid |
sentence |
| 22195962 |
Mitochondrial pdhk1 is tyrosine phosphorylated and activated by fgfr1 in cancer cells further mass spectrometric analysis identified three tyrosine residues of pdhk1, including y136, y243 and y244, that are phosphorylated by fgfr1 |
|
| Publications: |
3 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates
phosphorylation
|
FGFR1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98622 |
Tyr154 |
NRMPVAPyWTSPEKM |
Homo sapiens |
|
| pmid |
sentence |
| 8443592 |
Tyrosine residues 154 and 307, which are in the extracellular domain of transmembrane receptor isoforms and are in an unusual sequence context for tyrosine phosphorylation, were also phosphorylated. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98626 |
Tyr280 |
VEFMCKVySDPQPHI |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Fgfr signaling is under the control of tyrosine phosphorylation to elicit activation of cellular signaling cascades. Ligand binding induces receptor dimerization and transphosphorylation. Fgfr1 contains eleven tyrosine residues (tyr154, tyr280, tyr307, tyr463, tyr585, tyr605, tyr653, tyr654, tyr730 and tyr766), some of which are directly involved regulating the activity of the receptor and others bind to activate substrates leading to the activation of various transduction pathways. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98630 |
Tyr307 |
IGPDNLPyVQILKTA |
Homo sapiens |
|
| pmid |
sentence |
| 8443592 |
Tyrosine residues 154 and 307, which are in the extracellular domain of transmembrane receptor isoforms and are in an unusual sequence context for tyrosine phosphorylation, were also phosphorylated. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236179 |
Tyr463 |
MLAGVSEyELPEDPR |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235762 |
Tyr463 |
MLAGVSEyELPEDPR |
Rattus norvegicus |
Rat-1 Cell |
| pmid |
sentence |
| 19224897 |
This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235906 |
Tyr583 |
RRPPGLEyCYNPSHN |
Rattus norvegicus |
Rat-1 Cell |
| pmid |
sentence |
| 19224897 |
Autophosphorylation of Y653 is followed by the ordered autophosphorylation of several key tyrosine residues within binding sites for the SH2 or PTB domains of signaling proteins that bind to and are phosphorylated by activated FGFR1. This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236183 |
Tyr583 |
RRPPGLEyCYNPSHN |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236187 |
Tyr585 |
PPGLEYCyNPSHNPE |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235682 |
Tyr585 |
PPGLEYCyNPSHNPE |
Rattus norvegicus |
|
| pmid |
sentence |
| 19224897 |
Autophosphorylation of Y653 is followed by the ordered autophosphorylation of several key tyrosine residues within binding sites for the SH2 or PTB domains of signaling proteins that bind to and are phosphorylated by activated FGFR1. This second-stage autophosphorylation occurs on Y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of Y463 in the juxtamembrane region, Y766 in the C-terminal tail, and Y585 in the kinase insert region |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98634 |
Tyr605 |
KDLVSCAyQVARGME |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Fgfr signaling is under the control of tyrosine phosphorylation to elicit activation of cellular signaling cascades. Ligand binding induces receptor dimerization and transphosphorylation. Fgfr1 contains eleven tyrosine residues (tyr154, tyr280, tyr307, tyr463, tyr585, tyr605, tyr653, tyr654, tyr730 and tyr766), some of which are directly involved regulating the activity of the receptor and others bind to activate substrates leading to the activation of various transduction pathways. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236195 |
Tyr653 |
RDIHHIDyYKKTTNG |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1. We demonstrate that autophosphorylation on tyrosines 653 and 654 is important for activation of tyrosine kinase activity of fgfr1 and is therefore essential for fgfr1-mediated biological responses. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236199 |
Tyr654 |
DIHHIDYyKKTTNGR |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1. We demonstrate that autophosphorylation on tyrosines 653 and 654 is important for activation of tyrosine kinase activity of fgfr1 and is therefore essential for fgfr1-mediated biological responses. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-235686 |
Tyr730 |
SNCTNELyMMMRDCW |
Rattus norvegicus |
L-6 Myoblast Cell, PC-12 Cell |
| pmid |
sentence |
| 8622701 |
In this report, we describe the identification of six additional autophosphorylation sites (y-463, y-583, y-585, y-653, y-654 and y-730) on fgfr1.We have proposed that the role of the third stage of autophosphorylation is to enable the efficient tyrosine phosphorylation of substrate proteins that are physically bound to the receptor molecule by a maximally activated fgfr1 |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236191 |
Tyr730 |
SNCTNELyMMMRDCW |
Rattus norvegicus |
|
| pmid |
sentence |
| 19224897 |
Furthermore, under conditions in which wild-type or mutant FGFR1 are overexpressed, Y463, Y583, Y585, and Y730 are dispensable for tyrosine phosphorylation of Shc, the mitogen-activated protein kinase (MAPK) response, and stimulation of FGFR1-mediated cell proliferation and differentiation |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236203 |
Tyr766 |
ALTSNQEyLDLSMPL |
Rattus norvegicus |
|
| pmid |
sentence |
| 19224897 |
This second-stage autophosphorylation occurs on y583, in the kinase insert region (a noncatalytic sequence within the kinase domain), followed by autophosphorylation of y463 in the juxtamembrane region, y766 in the c-terminal tail, and y585 in the kinase insert region (1). The third-stage autophosphorylation takes place on the second tyrosine in the activation loop (y654), resulting in an additional 10-fold increase in the intrinsic tyrosine kinase activity of fgfr1. |
|
| Publications: |
15 |
Organism: |
Homo Sapiens, Rattus Norvegicus |
| Pathways: | Luminal Breast Cancer |
| + |
FGFR1 | down-regulates
phosphorylation
|
SYNCRIP |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98704 |
Tyr373 |
RVKKLKDyAFIHFDE |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Novel in vivo tyrosine phosphorylation sites were found in the fgfr-1, phospholipase cgamma, p90 ribosomal s6 kinase, cortactin, and ns-1-associated protein-1. Syncrip, was very recently found to be phosphorylated in response to insulin treatment of 3t3-l1 adipocytes (32). Phosphorylation of syncrip was accommodated by the insulin receptor tyrosine kinase in vitro but was inhibited upon binding of rna. Tyrosine phosphorylation at tyr-373 in the third rna recognition motif domain of nsap1/syncrip can possibly influence its rna binding properties and thus link fgfr-1 signaling to mrna metabolism. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates activity
phosphorylation
|
ACAT1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-264423 |
Tyr407 |
HALKQGEyGLASICN |
Homo sapiens |
NCI-H1299 Cell |
| pmid |
sentence |
| 27867011 |
Treatment with the FGFR1 inhibitor TKI258 in FGFR1-expressing H1299 cells led to decreased Y407 phosphorylation of ACAT1 in the mitochondrial fraction, where both ACAT1 and a fraction of FGFR1 were detected|Inhibition of tetrameric ACAT1 by abolishing Y407 phosphorylation or AH treatment results in decreased ACAT1 activity, |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | down-regulates
phosphorylation
|
CTTN |
0.318 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-98618 |
Tyr446 |
GTEPEPVySMEAADY |
Homo sapiens |
|
| pmid |
sentence |
| 12601080 |
Cortactin, which is an actin-binding protein that also plays a role in actin cytoskeleton dynamics (45), was phosphorylated on tyr-446 in our assay (by fgfr1).Phosphorylation of these residues attenuates the f-actin cross-linking activity |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | down-regulates activity
phosphorylation
|
PDP1 |
0.296 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-276640 |
Tyr94 |
SILKANEySFKVPEF |
Mus musculus |
NIH-3T3 Cell |
| pmid |
sentence |
| 24962578 |
Here we report that phosphorylation at another tyrosine residue, Tyr-94, inhibits PDP1 by reducing the binding ability of PDP1 to lipoic acid, which is covalently attached to the L2 domain of dihydrolipoyl acetyltransferase (E2) to recruit PDP1 to PDC. We found that multiple oncogenic tyrosine kinases directly phosphorylated PDP1 at Tyr-94, and Tyr-94 phosphorylation of PDP1 was common in diverse human cancer cells and primary leukemia cells from patients. |
|
| Publications: |
1 |
Organism: |
Mus Musculus |
| + |
2-Hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylic acid | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259703 |
|
|
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. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258183 |
|
|
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: |
2 |
Organism: |
In Vitro |
| + |
Brivanib alaninate | down-regulates
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190717 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates activity
phosphorylation
|
FRS2 |
0.863 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236944 |
|
|
Rattus norvegicus |
L-6 Myoblast Cell |
| pmid |
sentence |
| 9182757 |
In this report, we demonstrate that FGF stimulation induces tyrosine phosphorylation of a novel lipid anchored docking protein, termed FRS2, that forms a complex with Grb2/Sos, thus linking FGF-receptor activation to the Ras/MAPK signaling pathway. |
|
| Publications: |
1 |
Organism: |
Rattus Norvegicus |
| Pathways: | Luminal Breast Cancer |
| + |
pazopanib | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257735 |
|
|
Homo sapiens |
HUVEC Cell |
| pmid |
sentence |
| 18620382 |
Pyrimidine 13 showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50’s of 84, 74, 140, and 146 nM, respectively. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | down-regulates activity
chemical inhibition
|
Non-structural protein 2 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-260150 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18620382 |
Pyrimidine 13 showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFRβ, c-Kit, FGF-R1, and c-fms with IC50’s of 84, 74, 140, and 146 nM, respectively. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGF5 | up-regulates
binding
|
FGFR1 |
0.7 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-38704 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 8386828 |
Fgf-5 can bind and induce autophosphorylation of human fgf receptors (fgfr) 1 and 2. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
PD173074 | down-regulates
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-205725 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
BGJ-398 | down-regulates
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-190263 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
sorafenib tosylate | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259221 |
|
|
in vitro |
|
| pmid |
sentence |
| 16757355 |
Further characterization of sorafenib revealed that this molecule was a multikinase inhibitor that targeted the vascular endothelial growth factor receptor family (VEGFR-2 and VEGFR-3) and platelet-derived growth factor receptor family (PDGFR-beta and Kit), which play key roles in tumor progression and angiogenesis. The in vitro and cellular profile of sorafenib is summarized in Table I. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
regorafenib | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259177 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 26254357 |
A novel multi-kinase inhibitor, regorafenib (Figure 1), inhibits vascular endothelial growth factor receptor (VEGFR) 1, VEGFR2, and VEGFR3, that play key roles in angiogenesis, and fibroblast growth factor receptor (FGFR) 1, platelet-derived growth factor receptor-β (PDGFR-β), tyrosine kinase with immunoglobulin and epidermal growth factor homology domain 2 (TIE2) and the mutant oncogenic kinase KIT, RET, B-RAF |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
orantinib | down-regulates
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-207435 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| Other |
|
|
| Publications: |
1 |
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 |
| + |
FGF1 | up-regulates
binding
|
FGFR1 |
0.912 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-83143 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 11030354 |
Crystal structure of a ternary fgf-fgfr-heparin complex reveals a dual role for heparin in fgfr binding and dimerization. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Pathways: | Luminal Breast Cancer |
| + |
ponatinib | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259277 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23468082 |
Ponatinib is an oral multitargeted kinase inhibitor that potently inhibits all 4 members of the FGFR family. |
|
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-259276 |
|
|
Homo sapiens |
Non-small Cell Lung Cancer Cell |
| pmid |
sentence |
| 23563700 |
Ponatinib was able to significantly inhibit the growth of primary lung cancer cultures in vitro. Our data indicate that pharmacological inhibition of FGFR1 kinase activity with ponatinib may be effective for the treatment of lung cancer patients whose tumors overexpress FGFR1. |
|
| Publications: |
2 |
Organism: |
Homo Sapiens |
| + |
(2R)-1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methyl-6-pyrrolo[2,1-f][1,2,4]triazinyl]oxy]-2-propanol | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-258090 |
|
|
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 |
| + |
Gbeta | down-regulates
phosphorylation
|
FGFR1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-270013 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 23405013 |
Erk-mediated phosphorylation of fibroblast growth factor receptor 1 on ser777 inhibits signaling |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
nintedanib | down-regulates activity
chemical inhibition
|
FGFR1 |
0.8 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-257804 |
|
|
in vitro |
|
| pmid |
sentence |
| 18559524 |
In this report, we describe the preclinical profile of BIBF 1120, a combined VEGFR, FGFR, and PDGFR inhibitor currently entering phase III clinical studies in non–small cell lung carcinoma and other cancers. |
|
| Publications: |
1 |
Organism: |
In Vitro |
| + |
DUSP26 | down-regulates activity
dephosphorylation
|
FGFR1 |
0.2 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-277104 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 28701747 |
NEAP and DUSP26 dephosphorylated TrkA and FGFR1 directly.|We found that NEAP, but not its phosphatase-defective mutant, suppressed nerve growth factor (NGF) receptor TrkA and fibroblast growth factor receptor 1 (FGFR1) activation in PC12 cells |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| + |
FGFR1 | up-regulates
|
MEK1/2 |
0.315 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-244865 |
|
|
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 |
| Pathways: | Luminal Breast Cancer |
| + |
FGF1 | up-regulates activity
binding
|
FGFR1 |
0.912 |
| Identifier |
Residue |
Sequence |
Organism |
Cell Line |
| SIGNOR-236936 |
|
|
Homo sapiens |
|
| pmid |
sentence |
| 18940940 |
Together these data highlight the unique nature of the role of FGF-1 during the earliest stages of adipogenesis and establish a role for FGFR1 in human adipogenesis, identifying FGFR1 as a potential therapeutic target to reduce obesity. |
|
| Publications: |
1 |
Organism: |
Homo Sapiens |
| Tissue: |
Adipose Tissue |
| Pathways: | Luminal Breast Cancer |
3.0
FGFR1
- 
- 