Target

Ligand

Substrate

Meas. Tech.

HTRF Kinase Inhibition Assay

Citation

 Martin, MW; Newcomb, J; Nunes, JJ; McGowan, DC; Armistead, DM; Boucher, C; Buchanan, JL; Buckner, W; Chai, L; Elbaum, D; Epstein, LF; Faust, T; Flynn, S; Gallant, P; Gore, A; Gu, Y; Hsieh, F; Huang, X; Lee, JH; Metz, D; Middleton, S; Mohn, D; Morgenstern, K; Morrison, MJ; Novak, PM; Oliveira-dos-Santos, A; Powers, D; Rose, P; Schneider, S; Sell, S; Tudor, Y; Turci, SM; Welcher, AA; White, RD; Zack, D; Zhao, H; Zhu, L; Zhu, X; Ghiron, C; Amouzegh, P; Ermann, M; Jenkins, J; Johnston, D; Napier, S; Power, E Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity. J Med Chem 49:4981-91 (2006) [PubMed]  Article

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:

BDBM17744

Synonyms:

2,6-dimethylphenyl N-[2-({3,5-dimethoxy-4-[3-(4-methylpiperazin-1-yl)propoxy]phenyl}amino)pyrimidin-4-yl]-N-(2,4-dimethoxyphenyl)carbamate | 2-aminopyrimidine carbamate, 43

Type:

Small organic molecule

Emp. Form.:

C37H46N6O7

Mol. Mass.:

686.7971

SMILES:

COc1ccc(N(C(=O)Oc2c(C)cccc2C)c2ccnc(Nc3cc(OC)c(OCCCN4CCN(C)CC4)c(OC)c3)n2)c(OC)c1

Structure:

Search PDB for entries with ligand similarity:

Similarity to this molecule at least:

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:

ITINEEEEAYGWLDF