Target
Vascular endothelial growth factor receptor 2
Ligand
BDBM227926
Substrate
n/a
Meas. Tech.
KDR (VEGFR-2) Kinase Assay
pH
7±n/a
IC50
0.325±n/a nM
Comments
extracted
Citation
 Schall, AKlar, JLobell, MSchirok, HTelser, JMüller, SBrohm, DBriem, HJörißen, HKeldenich, JBöttger, MVon Degenfeld, GSchlange, TBömer, ULindner, NEilken, HHristodorov, DWasnaire, PGericke, KMBärfacker, L Substituted pyridobenzodiazepinone-derivatives and use thereof US Patent  US10047096 Publication Date 8/14/2018 
Target
Name:
Vascular endothelial growth factor receptor 2
Synonyms:
CD_antigen=CD309 | FLK1 | 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 | VGFR2_HUMAN | Vascular Endothelial Growth Factor Receptor Kinase 2 | Vascular endothelial growth factor receptor (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:
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLDWLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQDYRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWDSKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGEKLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRSDQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPPEIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVPPQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPYPCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGERVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPTPVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLTVLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNRNLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWLLLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPLGRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVNLLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLKRRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLASRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDRVYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTMLDCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVSCMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDSGMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYSSEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
  
Inhibitor
Name:
BDBM227926
Synonyms:
4-[(2-Fluoro-5-hydroxy-4-methylphenyl)amino]-8-{[(3-hydroxycyclobutyl)amino]methyl}-6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one | US10047096, 187
Type:
Small organic molecule
Emp. Form.:
C24H24FN5O3
Mol. Mass.:
449.4775
SMILES:
Cc1cc(F)c(Nc2ccnc3Nc4ccc(CNC5CC(O)C5)cc4NC(=O)c23)cc1O |(-9.65,3.64,;-8.32,2.87,;-8.32,1.33,;-6.99,.56,;-6.99,-.98,;-5.65,1.33,;-4.32,.56,;-4.32,-.98,;-5.65,-1.75,;-5.65,-3.29,;-4.32,-4.06,;-2.99,-3.29,;-1.78,-4.25,;-.28,-3.91,;.59,-5.18,;2.12,-5.06,;2.79,-3.68,;4.33,-3.68,;5.1,-2.34,;6.43,-1.57,;7.92,-1.97,;8.32,-.48,;9.65,.29,;6.83,-.09,;1.92,-2.41,;.39,-2.52,;-.28,-1.13,;-1.78,-.79,;-2.18,.7,;-2.99,-1.75,;-5.65,2.87,;-6.99,3.64,;-6.99,5.18,)|
Structure:
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