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Target
Angiopoietin-1 receptor
Ligand
BDBM14974
Substrate
Her2 Peptide Substrate
Meas. Tech.
Homogeneous Time-Resolved Fluorescence (HTRF) Enzyme Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
1±n/a nM
Citation
 Hodous, BL; Geuns-Meyer, SD; Hughes, PE; Albrecht, BK; Bellon, S; Bready, J; Caenepeel, S; Cee, VJ; Chaffee, SC; Coxon, A; Emery, M; Fretland, J; Gallant, P; Gu, Y; Hoffman, D; Johnson, RE; Kendall, R; Kim, JL; Long, AM; Morrison, M; Olivieri, PR; Patel, VF; Polverino, A; Rose, P; Tempest, P; Wang, L; Whittington, DA; Zhao, H Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J Med Chem 50:611-26 (2007) [PubMed]  Article 
Target
Name:
Angiopoietin-1 receptor
Synonyms:
TEK | TIE2 | TIE2_HUMAN | Tyrosine-protein kinase TIE-2 | Tyrosine-protein kinase receptor (TIE-2) | Tyrosine-protein kinase receptor TEK | Tyrosine-protein kinase receptor TEK (p140 TEK) | Tyrosine-protein kinase receptor TIE-2 | Tyrosine-protein kinase receptor TIE2/TEK | VMCM | VMCM1 | Vascular endothelial growth factor receptor 2 and tyrosine-protein kinase TIE-2 (KDR and TIE2) | p140 TEK
Type:
Enzyme
Mol. Mass.:
125835.70
Organism:
Homo sapiens (Human)
Description:
Q02763
Residue:
1124
Sequence:
MDSLASLVLCGVSLLLSGTVEGAMDLILINSLPLVSDAETSLTCIASGWRPHEPITIGRDFEALMNQHQDPLEVTQDVTREWAKKVVWKREKASKINGAYFCEGRVRGEAIRIRTMKMRQQASFLPATLTMTVDKGDNVNISFKKVLIKEEDAVIYKNGSFIHSVPRHEVPDILEVHLPHAQPQDAGVYSARYIGGNLFTSAFTRLIVRRCEAQKWGPECNHLCTACMNNGVCHEDTGECICPPGFMGRTCEKACELHTFGRTCKERCSGQEGCKSYVFCLPDPYGCSCATGWKGLQCNEACHPGFYGPDCKLRCSCNNGEMCDRFQGCLCSPGWQGLQCEREGIQRMTPKIVDLPDHIEVNSGKFNPICKASGWPLPTNEEMTLVKPDGTVLHPKDFNHTDHFSVAIFTIHRILPPDSGVWVCSVNTVAGMVEKPFNISVKVLPKPLNAPNVIDTGHNFAVINISSEPYFGDGPIKSKKLLYKPVNHYEAWQHIQVTNEIVTLNYLEPRTEYELCVQLVRRGEGGEGHPGPVRRFTTASIGLPPPRGLNLLPKSQTTLNLTWQPIFPSSEDDFYVEVERRSVQKSDQQNIKVPGNLTSVLLNNLHPREQYVVRARVNTKAQGEWSEDLTAWTLSDILPPQPENIKISNITHSSAVISWTILDGYSISSITIRYKVQGKNEDQHVDVKIKNATITQYQLKGLEPETAYQVDIFAENNIGSSNPAFSHELVTLPESQAPADLGGGKMLLIAILGSAGMTCLTVLLAFLIILQLKRANVQRRMAQAFQNVREEPAVQFNSGTLALNRKVKNNPDPTIYPVLDWNDIKFQDVIGEGNFGQVLKARIKKDGLRMDAAIKRMKEYASKDDHRDFAGELEVLCKLGHHPNIINLLGACEHRGYLYLAIEYAPHGNLLDFLRKSRVLETDPAFAIANSTASTLSSQQLLHFAADVARGMDYLSQKQFIHRDLAARNILVGENYVAKIADFGLSRGQEVYVKKTMGRLPVRWMAIESLNYSVYTTNSDVWSYGVLLWEIVSLGGTPYCGMTCAELYEKLPQGYRLEKPLNCDDEVYDLMRQCWREKPYERPSFAQILVSLNRMLEERKTYVNTTLYEKFTYAGIDCSAEEAA
  
Inhibitor
Name:
BDBM14974
Synonyms:
CHEMBL221484 | N-(3-(3-(Dimethylamino)propyl)-5-(trifluoromethyl)phenyl)-4-methyl-3-(3-(pyrimidin-4-yl)pyridin-2-ylamino)benzamide | N-{3-[3-(dimethylamino)propyl]-5-(trifluoromethyl)phenyl}-4-methyl-3-{[3-(pyrimidin-4-yl)pyridin-2-yl]amino}benzamide | pyridinyl pyrimidine 39
Type:
Small organic molecule
Emp. Form.:
C29H29F3N6O
Mol. Mass.:
534.5754
SMILES:
CN(C)CCCc1cc(NC(=O)c2ccc(C)c(Nc3ncccc3-c3ccncn3)c2)cc(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Her2 Peptide Substrate
Synonyms:
Biotinylated Her2 Peptide Substrate | biotinylated long chain peptide
Type:
Peptide
Mol. Mass.:
2278.65
Organism:
n/a
Description:
n/a
Residue:
20
Sequence:
ITINGGMEDIYFEFMGGKKK