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TargetVascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2)
LigandBDBM14971
Substrate/CompetitorGastrin Peptide Substrate
Meas. Tech.Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
pH7.5±n/a
Temperature296.15±n/a K
IC50 4.2±n/a nM
Citation Smith, ALDeMorin, FFParas, NAHuang, QPetkus, JKDoherty, EMNixey, TKim, JLWhittington, DAEpstein, LFLee, MRRose, MJBabij, CFernando, MHess, KLe, QBeltran, PCarnahan, J Selective inhibitors of the mutant B-Raf pathway: discovery of a potent and orally bioavailable aminoisoquinoline. J Med Chem52:6189-92 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2)
Name:Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2)
Synonyms:CD_antigen=CD309 | Fetal liver kinase 1 (FLK-1) | Flk-1/KDR | 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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BDBM14971
NameBDBM14971
Synonyms:4-Methyl-3-(3-(pyrimidin-4-yl)pyridin-2-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide | 4-methyl-3-{[3-(pyrimidin-4-yl)pyridin-2-yl]amino}-N-[3-(trifluoromethyl)phenyl]benzamide | JMC526189 Compound 2 | pyridinyl pyrimidine 6
TypeSmall organic molecule
Emp. Form.C24H18F3N5O
Mol. Mass.449.4278
SMILESCc1ccc(cc1Nc1ncccc1-c1ccncn1)C(=O)Nc1cccc(c1)C(F)(F)F
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
Gastrin Peptide Substrate
Name:Gastrin Peptide Substrate
Synonyms:Biotinylated gastrin peptide substrate | biotinylated gastrin substrate | gastrin substrate
Type:Peptide
Mol. Mass.:1823.88
Organism:n/a
Description:n/a
Residue:15
Sequence:
biotin-EEEEAYGWLDF