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TargetVascular endothelial growth factor receptor
LigandBDBM50015640
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1349477
IC50 442±n/a nM
Citation Jin, CHKrishnaiah, MSreenu, DSubrahmanyam, VBRao, KSLee, HJPark, SJPark, HJLee, KSheen, YYKim, DK Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF- type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem57:4213-38 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Vascular endothelial growth factor receptor
Name:Vascular endothelial growth factor receptor
Synonyms:CD_antigen=CD309 | Fetal liver kinase 1 (FLK-1) | Flk-1/KDR | Kinase Insert Domain Receptor | Protein-tyrosine kinase receptor Flk-1 | VEGFR kinase (KDR) | VEGFR-2 | VEGFR-2 (KDR) | VEGFR2 | Vascular Endothelial Growth Factor Receptor Kinase 2 | Vascular endothelial growth factor receptor (VEGFR-2) | Vascular endothelial growth factor receptor 2 (VEGFR-2) | Vascular endothelial growth factor receptor 2 (KDR) | Vascular endothelial growth factor receptor 2 (VEGFR-2) | Vascular endothelial growth factor receptor 2 (VEGFR2) | Vascular endothelial growth factor receptor 2 precursor (VEGFR-2) | Vascular endothelial growth factor receptor-2 (VEGFR-2)
Type:Receptor Tyrosine Kinase
Mol. Mass.:151510.97
Organism:Homo sapiens (human)
Description:P35968
Residue:1356
Sequence:
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD
WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD
YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD
SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE
KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS
DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP
EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP
PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY
PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE
RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT
PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT
VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR
NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL
LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL
GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN
LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK
RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA
SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR
VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML
DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS
CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS
GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS
SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
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  Blast E-value cutoff:
BDBM50015640
n/a
NameBDBM50015640
Synonyms:GALUNISERTIB | LY-2157299
TypeSmall organic molecule
Emp. Form.C22H19N5O
Mol. Mass.369.4192
SMILESCc1cccc(n1)-c1nn2CCCc2c1-c1ccnc2ccc(cc12)C(N)=O |(13.61,.14,;12.84,-1.19,;13.61,-2.53,;12.84,-3.86,;11.3,-3.86,;10.53,-2.53,;11.3,-1.19,;8.99,-2.53,;8.08,-1.28,;6.62,-1.76,;5.15,-1.28,;4.25,-2.53,;5.15,-3.77,;6.62,-3.3,;8.08,-3.77,;8.56,-5.24,;10.06,-5.56,;10.54,-7.02,;9.51,-8.17,;8,-7.85,;6.97,-8.99,;5.47,-8.67,;4.99,-7.21,;6.02,-6.06,;7.53,-6.38,;3.48,-6.89,;3.01,-5.42,;2.45,-8.03,)|
Structure
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