Proteins > Vascular endothelial growth factor receptor 1
Page last updated: 2024-08-07 16:04:17
Vascular endothelial growth factor receptor 1
A vascular endothelial growth factor receptor 1 that is encoded in the genome of human. [PRO:CNA]
Synonyms
VEGFR-1;
EC 2.7.10.1;
Fms-like tyrosine kinase 1;
FLT-1;
Tyrosine-protein kinase FRT;
Tyrosine-protein kinase receptor FLT;
FLT;
Vascular permeability factor receptor
Research
Bioassay Publications (107)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (0.93) | 18.2507 |
2000's | 44 (41.12) | 29.6817 |
2010's | 54 (50.47) | 24.3611 |
2020's | 8 (7.48) | 2.80 |
Compounds (118)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
pd 173074 | Homo sapiens (human) | IC50 | 0.1900 | 1 | 1 |
papaverine | Homo sapiens (human) | IC50 | 24.3300 | 1 | 1 |
whi p180 | Homo sapiens (human) | IC50 | 2.3300 | 3 | 5 |
galantamine | Homo sapiens (human) | IC50 | 0.5900 | 1 | 1 |
2,3,7,8-tetrachlorodibenzodioxine | Homo sapiens (human) | IC50 | 0.0027 | 1 | 0 |
2,3,7,8-tetrachlorodibenzodioxine | Homo sapiens (human) | Ki | 0.0007 | 1 | 0 |
staurosporine | Homo sapiens (human) | IC50 | 0.0149 | 7 | 7 |
ptk 787 | Homo sapiens (human) | IC50 | 0.0935 | 2 | 2 |
vatalanib | Homo sapiens (human) | IC50 | 0.1192 | 17 | 20 |
birb 796 | Homo sapiens (human) | IC50 | 0.6250 | 2 | 2 |
erlotinib | Homo sapiens (human) | IC50 | 0.2500 | 1 | 1 |
sorafenib | Homo sapiens (human) | IC50 | 0.0600 | 4 | 4 |
papaverinol | Homo sapiens (human) | IC50 | 10.7300 | 1 | 1 |
hematoxylin | Homo sapiens (human) | IC50 | 2.9000 | 1 | 1 |
zd 6474 | Homo sapiens (human) | IC50 | 0.5471 | 13 | 17 |
cb676475 | Homo sapiens (human) | IC50 | 9.5077 | 11 | 13 |
semaxinib | Homo sapiens (human) | IC50 | 0.7648 | 4 | 4 |
orantinib | Homo sapiens (human) | IC50 | 0.0280 | 1 | 1 |
su 11248 | Homo sapiens (human) | IC50 | 0.0458 | 2 | 2 |
su 11248 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
n,n'-dimethyl-n,n'-bis(mercaptoacetyl)hydrazine | Homo sapiens (human) | IC50 | 0.0320 | 1 | 1 |
6-(4-methoxyphenyl)-3-(3-thiophenyl)pyrazolo[1,5-a]pyrimidine | Homo sapiens (human) | IC50 | 0.3870 | 2 | 2 |
m475271 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
2-tert-butyl-9-fluoro-3,6-dihydro-7h-benz(h)imidazo(4,5-f)isoquinoline-7-one | Homo sapiens (human) | IC50 | 1.5200 | 1 | 1 |
2-((4-pyridyl)methyl)amino-n-(3-(trifluoromethyl)phenyl)benzamide | Homo sapiens (human) | IC50 | 0.1365 | 12 | 13 |
axitinib | Homo sapiens (human) | IC50 | 0.0001 | 2 | 2 |
gdp 366 | Homo sapiens (human) | IC50 | 0.0020 | 2 | 2 |
krn 633 | Homo sapiens (human) | IC50 | 0.0855 | 2 | 2 |
jnj 10198409 | Homo sapiens (human) | IC50 | 3.1000 | 1 | 1 |
lenvatinib | Homo sapiens (human) | IC50 | 0.0220 | 3 | 3 |
tivozanib | Homo sapiens (human) | IC50 | 0.0032 | 2 | 2 |
3,9-bis((ethylthio)methyl)-k-252a | Homo sapiens (human) | IC50 | 0.2090 | 1 | 1 |
cediranib | Homo sapiens (human) | IC50 | 0.0050 | 2 | 2 |
chir 99021 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
pazopanib | Homo sapiens (human) | IC50 | 0.0320 | 4 | 4 |
bibw 2992 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
aee 788 | Homo sapiens (human) | IC50 | 0.0590 | 1 | 1 |
saracatinib | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
exel-7647 | Homo sapiens (human) | IC50 | 0.0500 | 1 | 0 |
regorafenib | Homo sapiens (human) | IC50 | 0.0092 | 3 | 3 |
brivanib | Homo sapiens (human) | IC50 | 0.3800 | 1 | 1 |
brivanib | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
abt 869 | Homo sapiens (human) | IC50 | 0.0364 | 5 | 10 |
dorsomorphin | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
tak 285 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
crizotinib | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
chir-265 | Homo sapiens (human) | IC50 | 0.0200 | 1 | 1 |
motesanib | Homo sapiens (human) | IC50 | 0.8553 | 4 | 14 |
nvp-tae684 | Homo sapiens (human) | IC50 | 0.8720 | 1 | 1 |
tak 593 | Homo sapiens (human) | IC50 | 0.0032 | 2 | 2 |
ponatinib | Homo sapiens (human) | IC50 | 0.0123 | 2 | 2 |
quizartinib | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
lucitanib | Homo sapiens (human) | IC50 | 0.0070 | 3 | 3 |
cabozantinib | Homo sapiens (human) | IC50 | 0.0120 | 2 | 2 |
defactinib | Homo sapiens (human) | IC50 | 2.5000 | 1 | 0 |
gsk 1363089 | Homo sapiens (human) | IC50 | 0.2541 | 5 | 12 |
mk 2461 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
abt-348 | Homo sapiens (human) | IC50 | 0.0320 | 1 | 1 |
3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1h-imidazol-2-yl)methyl)benzamide | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
gsk 1070916 | Homo sapiens (human) | IC50 | 0.0420 | 2 | 1 |
chir 98014 | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
urmc-099 | Homo sapiens (human) | IC50 | 0.0390 | 1 | 1 |
pf-543 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
at 9283 | Homo sapiens (human) | IC50 | 0.0100 | 1 | 1 |
chir 258 | Homo sapiens (human) | IC50 | 0.0065 | 2 | 2 |
nintedanib | Homo sapiens (human) | IC50 | 0.0395 | 5 | 5 |
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
brivanib | Homo sapiens (human) | Activity | 0.0400 | 1 | 1 |
Tau Tubulin Kinase 1 (TTBK1), a new player in the fight against neurodegenerative diseases.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Discovery of the selective and efficacious inhibitors of FLT3 mutations.European journal of medicinal chemistry, , Jul-15, Volume: 155, 2018
Challenging clinically unresponsive medullary thyroid cancer: Discovery and pharmacological activity of novel RET inhibitors.European journal of medicinal chemistry, , Apr-25, Volume: 150, 2018
Novel LCK/FMS inhibitors based on phenoxypyrimidine scaffold as potential treatment for inflammatory disorders.European journal of medicinal chemistry, , Dec-01, Volume: 141, 2017
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.Bioorganic & medicinal chemistry, , 09-15, Volume: 27, Issue:18, 2019
Design, synthesis and in vitro antitumor activity of novel N-substituted-4-phenyl/benzylphthalazin-1-ones.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.Chemical biology & drug design, , Volume: 69, Issue:5, 2007
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 13, Issue:18, 2003
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction.Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 21, Issue:23, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.European journal of medicinal chemistry, , Aug-05, Volume: 156, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastatiBioorganic & medicinal chemistry, , Mar-01, Volume: 21, Issue:5, 2013
N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry, , Jan-15, Volume: 20, Issue:2, 2012
The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.Bioorganic & medicinal chemistry letters, , May-15, Volume: 20, Issue:10, 2010
Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.Bioorganic & medicinal chemistry, , May-15, Volume: 18, Issue:10, 2010
Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.Bioorganic & medicinal chemistry, , May-15, Volume: 16, Issue:10, 2008
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.Journal of natural products, , Apr-26, Volume: 76, Issue:4, 2013
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
[no title available]Journal of medicinal chemistry, , 04-22, Volume: 64, Issue:8, 2021
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.European journal of medicinal chemistry, , Jul-23, Volume: 82, 2014
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 22, Issue:15, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.Bioorganic & medicinal chemistry letters, , Dec-16, Volume: 12, Issue:24, 2002
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
3,4-Disubstituted isothiazoles: novel potent inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 19, Issue:4, 2009
ortho-Substituted azoles as selective and dual inhibitors of VEGF receptors 1 and 2.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Rational design of inhibitors that bind to inactive kinase conformations.Nature chemical biology, , Volume: 2, Issue:7, 2006
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 16, Issue:5, 2006
N-(Aryl)-4-(azolylethyl)thiazole-5-carboxamides: novel potent inhibitors of VEGF receptors I and II.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 16, Issue:6, 2006
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Recent developments in small molecule therapies for renal cell carcinoma.European journal of medicinal chemistry, , Dec-15, Volume: 142, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 16, Issue:16, 2006
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Design, synthesis and biological evaluation of deuterated Tivozanib for improving pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Discovery of Novel Pazopanib-Based HDAC and VEGFR Dual Inhibitors Targeting Cancer Epigenetics and Angiogenesis Simultaneously.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.Journal of medicinal chemistry, , Aug-14, Volume: 51, Issue:15, 2008
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development.Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Novel potent substituted 4-amino-2-thiopyrimidines as dual VEGFR-2 and BRAF kinase inhibitors.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry, , Jul-15, Volume: 19, Issue:14, 2011
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.ACS medicinal chemistry letters, , Sep-10, Volume: 6, Issue:9, 2015
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
De Novo Design at the Edge of Chaos.Journal of medicinal chemistry, , 05-12, Volume: 59, Issue:9, 2016
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts.Cancer research, , Sep-01, Volume: 66, Issue:17, 2006
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.Proceedings of the National Academy of Sciences of the United States of America, , Dec-11, Volume: 104, Issue:50, 2007
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.Proceedings of the National Academy of Sciences of the United States of America, , Jan-02, Volume: 104, Issue:1, 2007
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.Bioorganic & medicinal chemistry, , Apr-15, Volume: 21, Issue:8, 2013
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Discovery of 1-(4-(4-Amino-3-(4-(2-morpholinoethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)phenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea (CHMFL-FLT3-213) as a Highly Potent Type II FLT3 Kinase Inhibitor Capable of Overcoming a Variety of FLT3 Kinase MutanJournal of medicinal chemistry, , 10-26, Volume: 60, Issue:20, 2017
3-Phenyl-1H-5-pyrazolylamine-based derivatives as potent and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3).Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 22, Issue:14, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.Journal of medicinal chemistry, , Dec-10, Volume: 52, Issue:23, 2009
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Design, synthesis and biological evaluation of a series of novel 2-benzamide-4-(6-oxy-N-methyl-1-naphthamide)-pyridine derivatives as potent fibroblast growth factor receptor (FGFR) inhibitors.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFREuropean journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Design, synthesis and evaluation of sulfonylurea-containing 4-phenoxyquinolines as highly selective c-Met kinase inhibitors.Bioorganic & medicinal chemistry, , 07-01, Volume: 27, Issue:13, 2019
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
Recent advances in the development of dual VEGFR and c-Met small molecule inhibitors as anticancer drugs.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Design, synthesis and pharmacological evaluation of 6,7-disubstituted-4-phenoxyquinoline derivatives as potential antitumor agents.Bioorganic chemistry, , Volume: 57, 2014
Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors.Journal of medicinal chemistry, , Dec-27, Volume: 55, Issue:24, 2012
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
An overview of the binding models of FGFR tyrosine kinases in complex with small molecule inhibitors.European journal of medicinal chemistry, , Jan-27, Volume: 126, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Structural modifications of indolinones bearing a pyrrole moiety and discovery of a multi-kinase inhibitor with potent antitumor activity.Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
Evolution in medicinal chemistry of sorafenib derivatives for hepatocellular carcinoma.European journal of medicinal chemistry, , Oct-01, Volume: 179, 2019
Novel 6-methoxycarbonyl indolinones bearing a pyrrole Mannich base moiety as angiokinase inhibitors.Bioorganic & medicinal chemistry, , 03-15, Volume: 25, Issue:6, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, and evaluation of indolinones as triple angiokinase inhibitors and the discovery of a highly specific 6-methoxycarbonyl-substituted indolinone (BIBF 1120).Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy.Cancer research, , Jun-15, Volume: 68, Issue:12, 2008
Enables
This protein enables 6 target(s):
Target | Category | Definition |
transmembrane receptor protein tyrosine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP + a protein-L-tyrosine = ADP + a protein-L-tyrosine phosphate. [EC:2.7.10.1, GOC:mah] |
vascular endothelial growth factor receptor activity | molecular function | Combining with a vascular endothelial growth factor (VEGF) receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:mah, GOC:signaling, PMID:19909239] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
growth factor binding | molecular function | Binding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators] |
placental growth factor receptor activity | molecular function | Combining with placental growth factor (PlGF) receptor ligand and transmitting the signal across the plasma membrane to initiate a change in cell activity. [GOC:uh, PMID:12871269, PMID:7929268, Wikipedia:Placental_growth_factor] |
Located In
This protein is located in 5 target(s):
Target | Category | Definition |
extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
focal adhesion | cellular component | A cell-substrate junction that anchors the cell to the extracellular matrix and that forms a point of termination of actin filaments. In insects focal adhesion has also been referred to as hemi-adherens junction (HAJ). [GOC:aruk, GOC:bc, ISBN:0124325653, ISBN:0815316208, PMID:10419689, PMID:12191915, PMID:15246682, PMID:1643657, PMID:16805308, PMID:19197329, PMID:23033047, PMID:26923917, PMID:28796323, PMID:8314002] |
actin cytoskeleton | cellular component | The part of the cytoskeleton (the internal framework of a cell) composed of actin and associated proteins. Includes actin cytoskeleton-associated complexes. [GOC:jl, ISBN:0395825172, ISBN:0815316194] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
Target | Category | Definition |
receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 24 target(s):
Target | Category | Definition |
angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
monocyte chemotaxis | biological process | The movement of a monocyte in response to an external stimulus. [GOC:add, PMID:11696603, PMID:15173832] |
cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
positive regulation of phospholipase C activity | biological process | Any process that increases the rate of phospholipase C activity. [GOC:dph, GOC:tb] |
cell migration | biological process | The controlled self-propelled movement of a cell from one site to a destination guided by molecular cues. [GOC:cjm, GOC:dph, GOC:ems, GOC:pf, Wikipedia:Cell_migration] |
peptidyl-tyrosine phosphorylation | biological process | The phosphorylation of peptidyl-tyrosine to form peptidyl-O4'-phospho-L-tyrosine. [RESID:AA0039] |
cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
cellular response to vascular endothelial growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a vascular endothelial growth factor stimulus. [GOC:BHF, GOC:rl, PMID:18440775] |
vascular endothelial growth factor receptor-1 signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a vascular endothelial growth factor receptor-1 (VEGFR-1) on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:bf, GOC:uh, Wikipedia:FLT1, Wikipedia:VEGF_receptors] |
vascular endothelial growth factor signaling pathway | biological process | The series of molecular signals initiated by vascular endothelial growth factor (VEGF) binding its receptor on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, PMID:17470632] |
positive regulation of MAP kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of MAP kinase activity. [GOC:dph, GOC:go_curators] |
positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
protein autophosphorylation | biological process | The phosphorylation by a protein of one or more of its own amino acid residues (cis-autophosphorylation), or residues on an identical protein (trans-autophosphorylation). [ISBN:0198506732] |
vascular endothelial growth factor receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a vascular endothelial growth factor receptor (VEGFR) on the surface of the target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
blood vessel morphogenesis | biological process | The process in which the anatomical structures of blood vessels are generated and organized. The blood vessel is the vasculature carrying blood. [GOC:jid] |
embryonic morphogenesis | biological process | The process in which anatomical structures are generated and organized during the embryonic phase. The embryonic phase begins with zygote formation. The end of the embryonic phase is organism-specific. For example, it would be at birth for mammals, larval hatching for insects and seed dormancy in plants. [GOC:jid, GOC:mtg_sensu] |
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
negative regulation of vascular endothelial cell proliferation | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of vascular endothelial cell proliferation. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:nc, GOC:TermGenie, PMID:23201774] |
hyaloid vascular plexus regression | biological process | The developmental process in which the hyaloid vascular plexus is destroyed as a part of its normal progression. [GOC:hjd, PMID:18841878] |
multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |
positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |