Target

Ligand

Substrate

Meas. Tech.

HTRF Kinase Inhibition Assay

Citation

 DiMauro, EF; Newcomb, J; Nunes, JJ; Bemis, JE; Boucher, C; Chai, L; Chaffee, SC; Deak, HL; Epstein, LF; Faust, T; Gallant, P; Gore, A; Gu, Y; Henkle, B; Hsieh, F; Huang, X; Kim, JL; Lee, JH; Martin, MW; McGowan, DC; Metz, D; Mohn, D; Morgenstern, KA; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, PE; Schneider, S; Tomlinson, SA; Tudor, YY; Turci, SM; Welcher, AA; Zhao, H; Zhu, L; Zhu, X Structure-guided design of aminopyrimidine amides as potent, selective inhibitors of lymphocyte specific kinase: synthesis, structure-activity relationships, and inhibition of in vivo T cell activation. J Med Chem 51:1681-94 (2008) [PubMed]  Article Copy BDB DOI

More Info.:

Get all data from this article,   Solution Info,  Assay Method

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

Blast this sequence in BindingDB or PDB

  
Blast E-value cutoff:

Name:

BDBM26375

Synonyms:

4-methyl-3-N-(2-{[2-(morpholin-4-yl)ethyl]amino}pyrimidin-5-yl)-1-N-[3-(trifluoromethyl)benzene]benzene-1,3-dicarboxamide | Aminopyrimidine amide, 13e

Type:

Small organic molecule

Emp. Form.:

C26H27F3N6O3

Mol. Mass.:

528.5262

SMILES:

Cc1ccc(NC(=O)c2cccc(c2)C(F)(F)F)cc1C(=O)Nc1cnc(NCCN2CCOCC2)nc1

Structure:

Search PDB for entries with ligand similarity:

Similarity to this molecule at least:

Name:

biotinylated gastrin substrate

Synonyms:

n/a

Type:

Peptide

Mol. Mass.:

2100.22

Organism:

n/a

Description:

n/a

Residue:

17

Sequence:

ITINYLEEEEAYGWLDF