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Target
Angiopoietin-1 receptor
Ligand
BDBM8846
Substrate
biotinylated poly(Glu-Tyr)
Meas. Tech.
Homogeneous Time-resolved Fluorescence (HTRF) Assay
IC50
17±n/a nM
Citation
 Dai, Y; Guo, Y; Frey, RR; Ji, Z; Curtin, ML; Ahmed, AA; Albert, DH; Arnold, L; Arries, SS; Barlozzari, T; Bauch, JL; Bouska, JJ; Bousquet, PF; Cunha, GA; Glaser, KB; Guo, J; Li, J; Marcotte, PA; Marsh, KC; Moskey, MD; Pease, LJ; Stewart, KD; Stoll, VS; Tapang, P; Wishart, N; Davidsen, SK; Michaelides, MR Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors. J Med Chem 48:6066-83 (2005) [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:
BDBM8846
Synonyms:
3-(4-{4-amino-6-methylthieno[2,3-d]pyrimidin-5-yl}phenyl)-1-[2-fluoro-5-(trifluoromethyl)phenyl]urea | N-[4-(4-Amino-6-methylthieno[2,3-d]pyrimidin-5-yl)-phenyl]-N -[2-fluoro-5-(trifluoromethyl)phenyl]urea | Thienopyrimidine deriv. 28
Type:
Small organic molecule
Emp. Form.:
C21H15F4N5OS
Mol. Mass.:
461.435
SMILES:
Cc1sc2ncnc(N)c2c1-c1ccc(NC(=O)Nc2cc(ccc2F)C(F)(F)F)cc1
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
biotinylated poly(Glu-Tyr)
Synonyms:
n/a
Type:
Random Copolymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
n/a
Residue:
3
Sequence:
NA