General Information of the Protein
Protein ID
PT00925
Protein Name
Vascular endothelial growth factor receptor 3
Secondarily
Protein Name
Fms-like tyrosine kinase 4
Tyrosine-protein kinase receptor FLT4
Gene Name
FLT4
Secondarily
Gene Name
VEGFR3
Sequence
MQRGAALCLRLWLCLGLLDGLVSGYSMTPPTLNITEESHVIDTGDSLSISCRGQHPLEWAWPGAQEAPATGDKDSEDTGVVRDCEGTDARPYCKVLLLHEVHANDTGSYVCYYKYIKARIEGTTAASSYVFVRDFEQPFINKPDTLLVNRKDAMWVPCLVSIPGLNVTLRSQSSVLWPDGQEVVWDDRRGMLVSTPLLHDALYLQCETTWGDQDFLSNPFLVHITGNELYDIQLLPRKSLELLVGEKLVLNCTVWAEFNSGVTFDWDYPGKQAERGKWVPERRSQQTHTELSSILTIHNVSQHDLGSYVCKANNGIQRFRESTEVIVHENPFISVEWLKGPILEATAGDELVKLPVKLAAYPPPEFQWYKDGKALSGRHSPHALVLKEVTEASTGTYTLALWNSAAGLRRNISLELVVNVPPQIHEKEASSPSIYSRHSRQALTCTAYGVPLPLSIQWHWRPWTPCKMFAQRSLRRRQQQDLMPQCRDWRAVTTQDAVNPIESLDTWTEFVEGKNKTVSKLVIQNANVSAMYKCVVSNKVGQDERLIYFYVTTIPDGFTIESKPSEELLEGQPVLLSCQADSYKYEHLRWYRLNLSTLHDAHGNPLLLDCKNVHLFATPLAASLEEVAPGARHATLSLSIPRVAPEHEGHYVCEVQDRRSHDKHCHKKYLSVQALEAPRLTQNLTDLLVNVSDSLEMQCLVAGAHAPSIVWYKDERLLEEKSGVDLADSNQKLSIQRVREEDAGRYLCSVCNAKGCVNSSASVAVEGSEDKGSMEIVILVGTGVIAVFFWVLLLLIFCNMRRPAHADIKTGYLSIIMDPGEVPLEEQCEYLSYDASQWEFPRERLHLGRVLGYGAFGKVVEASAFGIHKGSSCDTVAVKMLKEGATASEHRALMSELKILIHIGNHLNVVNLLGACTKPQGPLMVIVEFCKYGNLSNFLRAKRDAFSPCAEKSPEQRGRFRAMVELARLDRRRPGSSDRVLFARFSKTEGGARRASPDQEAEDLWLSPLTMEDLVCYSFQVARGMEFLASRKCIHRDLAARNILLSESDVVKICDFGLARDIYKDPDYVRKGSARLPLKWMAPESIFDKVYTTQSDVWSFGVLLWEIFSLGASPYPGVQINEEFCQRLRDGTRMRAPELATPAIRRIMLNCWSGDPKARPAFSELVEILGDLLQGRGLQEEEEVCMAPRSSQSSEEGSFSQVSTMALHIAQADAEDSPPSLQRHSLAARYYNWVSFPGCLARGAETRGSSRMKTFEEFPMTPTTYKGSVDNQTDSGMVLASEEFEQIESRHRQESGFSCKGPGQNVAVTRAHPDSQGRRRRPERGARGGQVFYNSEYGELSEPSEEDHCSPSARVTFFTDNSY
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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 VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardiovascular system during embryonic development. Promotes proliferation, survival and migration of endothelial cells, and regulates angiogenic sprouting. Signaling by activated FLT4 leads to enhanced production of VEGFC, and to a lesser degree VEGFA, thereby creating a positive feedback loop that enhances FLT4 signaling. Modulates KDR signaling by forming heterodimers. The secreted isoform 3 may function as a decoy receptor for VEGFC and/or VEGFD and play an important role as a negative regulator of VEGFC-mediated lymphangiogenesis and angiogenesis. Binding of vascular growth factors to isoform 1 or isoform 2 leads to the activation of several signaling cascades; isoform 2 seems to be less efficient in signal transduction, because it has a truncated C-terminus and therefore lacks several phosphorylation sites. Mediates activation of the MAPK1/ERK2, MAPK3/ERK1 signaling pathway, of MAPK8 and the JUN signaling pathway, and of the AKT1 signaling pathway. Phosphorylates SHC1. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase. Promotes phosphorylation of MAPK8 at 'Thr-183' and 'Tyr-185', and of AKT1 at 'Ser-473'.
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Uniprot ID
Primary ID:
P35916

Secondarily ID:
A8K6L4
B5A926
Q16067
Q86W07
Q86W08
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Ensembl ID
ENSG00000037280
HGNC ID
HGNC:3767
Subcellular Location
Cell membrane
Cytoplasm
Nucleus
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: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0645833
(3S,8S,9S)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10,11,12-hexahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione
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C19H24O7
 1
1
GI50 = 50 nM
   TI
   LI
   LO
   TS
CP0263163
2-amino-1-ethyl-7-[(3R)-3-hydroxy-4-methoxy-3-methylbut-1-ynyl]-N-methyl-4-oxo-1,8-naphthyridine-3-carboxamide
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C18H22N4O4
 1
1
GI50 = 59 nM
   TI
   LI
   LO
   TS
CP0139586
(10S,12Z,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1
GI50 = 79 nM
   TI
   LI
   LO
   TS
CP0558016
(10S,12Z,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1
GI50 = 96 nM
   TI
   LI
   LO
   TS
CP0263164
(10S,11E,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,11,17,19-heptaene-8,14-dione
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C22H22O7
 1
1
GI50 = 130 nM
   TI
   LI
   LO
   TS
CP0249330
(10S,12Z)-6-hydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(20),2(7),3,5,12,17(21),18-heptaene-8,14-dione
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C22H22O5
 1
1
GI50 = 240 nM
   TI
   LI
   LO
   TS
CP0421231
N-[[1-[4-[[3-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]carbamoylamino]-2-(trifluoromethyl)phenyl]piperidin-4-yl]methyl]propanamide
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C34H36F3N5O5
 1
1
GI50 = 240 nM
   TI
   LI
   LO
   TS
CP0139006
(10S,12Z,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1
GI50 = 880 nM
   TI
   LI
   LO
   TS
CP0139002
(10S,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1
GI50 = 2200 nM
   TI
   LI
   LO
   TS
CP0165545
(10S,12Z,15R,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-14-methylidene-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C23H24O6
 1
1
GI50 > 25000 nM
   TI
   LI
   LO
   TS
CP0202493
(10S,12Z,14R,15R,16R)-6,14,15,16-tetrahydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C22H24O7
 1
1
GI50 > 25000 nM
   TI
   LI
   LO
   TS
CP0202494
(10S,12Z,14S,15R,16R)-14-amino-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C22H25NO6
 1
1
GI50 > 25000 nM
   TI
   LI
   LO
   TS
CP0356481
(10S,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1
GI50 > 25000 nM
   TI
   LI
   LO
   TS
CP0531968
(10S,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1
GI50 > 25000 nM
   TI
   LI
   LO
   TS
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
 1
1
IC50 = 2072 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0645833
(3S,8S,9S)-8,9,16-trihydroxy-14-methoxy-3-methyl-3,4,9,10,11,12-hexahydro-1H-benzo[c][1]oxacyclotetradecine-1,7(8H)-dione
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C19H24O7
 2
1 IC50 = 0.73 nM
2 IC50 = 1.13 nM
CP0164714
US9238644, 16
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C27H31ClN6O
 1
1 IC50 = 1 nM
CP0139586
(10S,12Z,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1 IC50 = 1.1 nM
CP0263163
2-amino-1-ethyl-7-[(3R)-3-hydroxy-4-methoxy-3-methylbut-1-ynyl]-N-methyl-4-oxo-1,8-naphthyridine-3-carboxamide
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C18H22N4O4
 1
1 IC50 = 1.2 nM
CP0318937
US9238644, 24
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C29H34ClN5O3
 1
1 IC50 = 2 nM
CP0244017
US9238644, 19
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C19H19ClN6O
 1
1 IC50 = 3 nM
CP0250342
US9238644, 18
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C25H30ClN7O
 1
1 IC50 = 3 nM
CP0438251
US9238644, 45
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C20H23ClN6O
 1
1 IC50 = 3 nM
CP0419578
US9238644, 13
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C20H21ClN6O
 1
1 IC50 = 4 nM
CP0438249
US9238644, 14
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C22H24ClN7O
 1
1 IC50 = 6 nM
CP0272870
US9238644, 20
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C23H26ClN7O
 1
1 IC50 = 7 nM
CP0314616
US9238644, 21
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C24H28ClN7O
 1
1 IC50 = 7 nM
CP0313365
US9238644, 6
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C21H20ClN5O
 1
1 IC50 = 8 nM
CP0331578
US9238644, 64
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C23H22F3N5O2
 1
1 IC50 = 8 nM
CP0314615
US9238644, 17
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C24H28ClN7O
 1
1 IC50 = 9 nM
CP0559808
US9238644, 44
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C24H30ClN7O
 1
1 IC50 = 9 nM
CP0559883
US9238644, 3
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C29H32F3N5O
 1
1 IC50 = 9 nM
CP0807372
US9238644, 35
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C18H19ClN6O
 1
1 IC50 = 9 nM
CP0139006
(10S,12Z,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1 IC50 = 9.2 nM
CP0263164
(10S,11E,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,11,17,19-heptaene-8,14-dione
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C22H22O7
 1
1 IC50 = 9.9 nM
CP0266397
US9238644, 8
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C28H32ClN5O
 1
1 IC50 = 10 nM
CP0342880
US9238644, 2
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C28H30F3N5O
 1
1 IC50 = 10 nM
CP0515208
US9238644, 7
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C27H30ClN5O
 1
1 IC50 = 10 nM
CP0318933
US9238644, 15
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C26H29ClN6O
 1
1 IC50 = 11 nM
CP0272833
US9238644, 51
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C20H24N6O
 1
1 IC50 = 15 nM
CP0559807
US9238644, 36
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C19H21ClN6O
 1
1 IC50 = 16 nM
CP0490075
US9238644, 4
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C26H26F3N5O
 1
1 IC50 = 22 nM
CP0558016
(10S,12Z,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaene-8,14-dione
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C22H22O7
 1
1 IC50 = 23 nM
CP0158674
US9238644, 56
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C24H28F3N7O
 1
1 IC50 = 27 nM
CP0483298
US9238644, 57
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C25H30F3N7O
 1
1 IC50 = 27 nM
CP0249330
(10S,12Z)-6-hydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(20),2(7),3,5,12,17(21),18-heptaene-8,14-dione
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C22H22O5
 1
1 IC50 = 27 nM
CP0132099
US9238644, 12
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C20H19ClN6O
 1
1 IC50 = 39 nM
CP0514645
US9238644, 1-2A
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C28H32F3N5O
 1
1 IC50 = 75 nM
CP0435116
US9238644, 1
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C28H32F3N5O
 1
1 IC50 = 91 nM
CP0342879
US9238644, 1-1A
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C28H32F3N5O
 1
1 IC50 = 103 nM
CP0015507
2-(4-(6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
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C30H31N5O3S
 1
1 IC50 = 121 nM
CP0016366
2-(4-(6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yloxy)phenyl)benzo[d]thiazole
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C29H28N4O3S
 1
1 IC50 = 140 nM
CP0015511
2-[3-fluoro-4-[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]oxyphenyl]-1,3-benzothiazole
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C30H30FN5O3S
 1
1 IC50 = 190 nM
CP0139002
(10S,15R,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1 IC50 = 190 nM
CP0061157
N-[4-(1,3-benzothiazol-2-yl)-3-fluorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 210 nM
CP0151244
N-[4-(1,3-benzothiazol-2-yl)-2-fluorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 350 nM
CP0166275
N-[4-(1,3-benzothiazol-2-yl)-3-chlorophenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31ClN6O2S
 1
1 IC50 = 470 nM
CP0151301
2-(1,3-benzothiazol-2-yl)-5-[[6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-yl]amino]phenol
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C30H32N6O3S
 1
1 IC50 = 520 nM
CP0069712
N-[4-(6-fluoro-1,3-benzothiazol-2-yl)phenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31FN6O2S
 1
1 IC50 = 865 nM
CP0091117
N-[4-(5-chloro-1,3-benzothiazol-2-yl)phenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C30H31ClN6O2S
 1
1 IC50 = 1300 nM
CP0151259
N-[4-(1,3-benzothiazol-2-yl)-2-methoxyphenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C31H34N6O3S
 1
1 IC50 = 1700 nM
CP0531968
(10S,15S,16S)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1 IC50 = 5300 nM
CP0135618
N-[4-(1,3-benzothiazol-2-yl)-3-methoxyphenyl]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazolin-4-amine
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C31H34N6O3S
 1
1 IC50 = 7100 nM
CP0128578
6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]-N-[4-[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]phenyl]quinazolin-4-amine
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C31H31F3N6O2S
 1
1 IC50 > 10000 nM
CP0165545
(10S,12Z,15R,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-14-methylidene-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C23H24O6
 1
1 IC50 > 10000 nM
CP0202493
(10S,12Z,14R,15R,16R)-6,14,15,16-tetrahydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C22H24O7
 1
1 IC50 > 10000 nM
CP0202494
(10S,12Z,14S,15R,16R)-14-amino-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,12,17,19-heptaen-8-one
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C22H25NO6
 1
1 IC50 > 10000 nM
CP0356481
(10S,15S,16R)-6,15,16-trihydroxy-4-methoxy-10-methyl-9-oxatricyclo[15.3.1.02,7]henicosa-1(21),2(7),3,5,17,19-hexaene-8,14-dione
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C22H24O7
 1
1 IC50 > 10000 nM
Clinical Information about the Protein
Target 1 ( Vascular endothelial growth factor receptor 3 (FLT-4) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Renal cell carcinoma [ICD-11: 2C90]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Alzheimer disease [ICD-11: 8A20]
Approved Drug(s) 1 Approved Drug  1
1 Tivozanib Approved
Renal cell carcinoma
Clinical Trial Drug(s) 6 Clinical Trial Drugs  6
1 ABT-869 Phase 3
Solid tumour/cancer
2 E-3810 Phase 3
Solid tumour/cancer
3 Famitinib Phase 2
Solid tumour/cancer
4 VATALANIB Phase 2
Solid tumour/cancer
5 MGCD516 Phase 2/3
Solid tumour/cancer
6 MK-2461 Phase 1/2
Alzheimer disease
Investigative Drug(s) 1 Investigative Drug  1
1 SAR-131675 Investigative
Solid tumour/cancer