General Information of the Protein
Protein ID
PT01142
Protein Name
Vascular endothelial growth factor receptor 1
Secondarily
Protein Name
Fms-like tyrosine kinase 1
Tyrosine-protein kinase FRT
Tyrosine-protein kinase receptor FLT
Vascular permeability factor receptor
Gene Name
FLT1
Secondarily
Gene Name
FLT
FRT
VEGFR1
Sequence
MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHKWSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKETESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPDGKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPVKLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDKMQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVKAFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTATLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARCDFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNKVGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTMHYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEAPYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIERVTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFIRKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGKVVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTKQGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSVTSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIHRDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKSDVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRDPKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISAPKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTWTDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIACCSPPPDYNSVVLYSTPPI
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase VEGFR family
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. Acts as a positive regulator of postnatal retinal hyaloid vessel regression (By similarity). May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. Can promote endothelial cell proliferation, survival and angiogenesis in adulthood. Its function in promoting cell proliferation seems to be cell-type specific. Promotes PGF-mediated proliferation of endothelial cells, proliferation of some types of cancer cells, but does not promote proliferation of normal fibroblasts (in vitro). Has very high affinity for VEGFA and relatively low protein kinase activity; may function as a negative regulator of VEGFA signaling by limiting the amount of free VEGFA and preventing its binding to KDR. Modulates KDR signaling by forming heterodimers with KDR. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leading to activation of phosphatidylinositol kinase and the downstream signaling pathway. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Phosphorylates SRC and YES1, and may also phosphorylate CBL. Promotes phosphorylation of AKT1 at 'Ser-473'. Promotes phosphorylation of PTK2/FAK1 (PubMed:16685275).
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Uniprot ID
Primary ID:
P17948

Secondarily ID:
A3E342
A3E344
A8KA71
B0LPF1
B2BF46
B2BF47
B2BF48
B3FR89
B5A923
F5H5L6
O60722
P16057
Q12954
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Ensembl ID
ENSG00000102755
HGNC ID
HGNC:3763
Subcellular Location
Cell membrane
Endosome
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000073 , A-498
Compound ID Compound Name Compound Formula
CP0063796
Anilinoquinazoline deriv. 4
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C16H13ClFN3O2
 2
1
IC50 = 14100 nM
   TI
   LI
   LO
   TS
2
IC50 = 17700 nM
   TI
   LI
   LO
   TS
CP0395235
4-N-(4-chlorophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C21H20ClN5O2
 1
1
IC50 = 15200 nM
   TI
   LI
   LO
   TS
CP0126790
4-N-(3-bromophenyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C23H18BrN5
 1
1
IC50 = 16000 nM
   TI
   LI
   LO
   TS
CP0392884
4-N-(4-chloro-2-fluorophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C20H17ClFN5
 1
1
IC50 = 19200 nM
   TI
   LI
   LO
   TS
CP0096083
4-N-(3-bromophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C21H20BrN5O2
 2
1
IC50 = 31100 nM
   TI
   LI
   LO
   TS
2
IC50 = 45900 nM
   TI
   LI
   LO
   TS
CP0391385
4-N-(4-chlorophenyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C23H18ClN5
 1
1
IC50 = 31100 nM
   TI
   LI
   LO
   TS
CP0167979
4-N-(3-bromophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C20H18BrN5
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0275218
4-N-(3-bromophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H14BrCl2N5
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0410666
4-N-(3-bromophenyl)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H17BrN6
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0418813
4-N-(3-bromophenyl)-7-(naphthalen-2-ylmethyl)pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C23H18BrN5
 1
1
IC50 = 50800 nM
   TI
   LI
   LO
   TS
CP0400032
4-N-(4-chloro-2-fluorophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H13Cl3FN5
 1
1
IC50 = 70900 nM
   TI
   LI
   LO
   TS
CP0402192
4-N-(3-bromophenyl)-7-[(4-chlorophenyl)methyl]pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H15BrClN5
 1
1
IC50 = 79900 nM
   TI
   LI
   LO
   TS
CP0417588
4-N-(3-bromo-4-fluorophenyl)-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H16BrFN6
 1
1
IC50 = 93600 nM
   TI
   LI
   LO
   TS
CP0437754
7-benzyl-4-N-(3-bromophenyl)pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H16BrN5
 1
1
IC50 = 99300 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0019908
BDBM50242742
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C30H40ClN7O3S
 2
1 EC50 = 872 nM
2 Kd = 550 nM
CP0036099
1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methyl-phenyl)urea
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C21H18FN5O
 3
1 IC50 = 3 nM
2 IC50 = 70 nM
3 Kd = 7.5 nM
CP0251838
US9340555, 15
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C31H34FN5O4S
 1
1 IC50 = 3 nM
CP0274646
US9340555, 70
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C29H32FN5O3S
 1
1 IC50 = 3 nM
CP0173795
US9340555, 12
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C26H23FN8O3S
 1
1 IC50 = 4 nM
CP0132770
US9340555, 69
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C28H30FN5O3S
 1
1 IC50 = 5 nM
CP0173796
US9340555, 14
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C33H37FN6O5S
 1
1 IC50 = 5 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 7
1 IC50 = 5.4 nM
2 IC50 = 6.31 nM
3 IC50 = 8.19 nM
4 IC50 = 14.7 nM
5 IC50 = 15.97 nM
6 IC50 = 19 nM
7 Kd = 150 nM
CP0117058
US9340555, 34
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C30H32F2N6O3S
 1
1 IC50 = 6 nM
CP0325013
US9340555, 18
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C28H28FN5O5S
 1
1 IC50 = 6 nM
CP0008706
(3Z)-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2,3-dihydro-1H-indol-2-one
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C15H14N2O
 2
1 IC50 = 8 nM
2 IC50 = 43 nM
CP0129158
US9340555, 25
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C28H27F2N5O5S
 1
1 IC50 = 8 nM
CP0264790
US9340555, 28
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C28H24F2N4O5S
 1
1 IC50 = 8 nM
CP0242332
US9340555, 31
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C27H25F2N5O5S
 1
1 IC50 = 9 nM
CP0264788
US9340555, 19
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C31H32FN5O7S
 1
1 IC50 = 9 nM
CP0340984
US9340555, 24
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C32H34F2N6O5S
 1
1 IC50 = 9 nM
CP0098371
US9340555, 13
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C25H21FN8O3S
 1
1 IC50 = 10 nM
CP0118006
US9340555, 16
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C30H32FN5O5S
 1
1 IC50 = 10 nM
CP0132764
US9340555, 17
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C31H32FN5O6S
 1
1 IC50 = 10 nM
CP0243641
US9340555, 26
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C31H31F2N5O7S
 1
1 IC50 = 10 nM
CP0561541
US9340555, 29
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C36H39F2N7O6S
 1
1 IC50 = 10 nM
CP0132767
US9340555, 32
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C24H21F2N5O3S
 1
1 IC50 = 11 nM
CP0187568
US9340555, 27
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C30H29F2N5O7S
 1
1 IC50 = 11 nM
CP0450031
US9340555, 23
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C31H32F2N6O5S
 1
1 IC50 = 13 nM
CP0018477
4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
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C21H16ClF3N4O3
 4
1 IC50 = 26 nM
2 IC50 = 31 nM
3 IC50 = 165 nM
4 Kd = 31 nM
CP0484070
US9340555, 33
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C29H29F2N5O5S
 1
1 IC50 = 60 nM
CP0561557
US9340555, 30
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C30H29F2N5O5S
 1
1 IC50 = 112 nM
CP0035016
1-[2-chloro-4-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-propylurea
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C20H21ClN4O4
 1
1 IC50 = 170 nM
CP0063796
Anilinoquinazoline deriv. 4
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C16H13ClFN3O2
 2
1 IC50 = 2000 nM
2 IC50 = 17700 nM
CP0126790
4-N-(3-bromophenyl)-6-(naphthalen-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C23H18BrN5
 1
1 IC50 = 19200 nM
CP0096083
4-N-(3-bromophenyl)-6-[(2,5-dimethoxyphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C21H20BrN5O2
 1
1 IC50 = 31100 nM
CP0167979
4-N-(3-bromophenyl)-6-[(2-methylphenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C20H18BrN5
 1
1 IC50 > 50000 nM
CP0275218
4-N-(3-bromophenyl)-6-[(2,4-dichlorophenyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamine
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C19H14BrCl2N5
 1
1 IC50 > 50000 nM
Clinical Information about the Protein
Target 1 ( VEGFR1 messenger RNA (VEGFR1 mRNA) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Thrombocytopenia [ICD-11: 3B64]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Alzheimer disease [ICD-11: 8A20]
Approved Drug(s) 1 Approved Drug  1
1 Romiplostim Approved
Thrombocytopenia
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 VATALANIB Phase 2
Solid tumour/cancer
2 MK-2461 Phase 1/2
Alzheimer disease
Target 2 ( Vascular endothelial growth factor receptor 1 (FLT-1) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Renal cell carcinoma [ICD-11: 2C90]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s) 1 Approved Drug  1
1 Tivozanib Approved
Renal cell carcinoma
Clinical Trial Drug(s) 3 Clinical Trial Drugs  3
1 E-3810 Phase 3
Solid tumour/cancer
2 Famitinib Phase 2
Solid tumour/cancer
3 CEP-11981 Phase 1
Solid tumour/cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT02141 Vascular endothelial growth factor receptor 1 Mus musculus, Mouse