Target
Angiopoietin-1 receptor
Ligand
BDBM14983
Substrate
n/a
Meas. Tech.
ChEMBL_540209 (CHEMBL1029838)
IC50
10±n/a nM
Citation
 Cee, VJCheng, ACRomero, KBellon, SMohr, CWhittington, DABak, ABready, JCaenepeel, SCoxon, ADeak, HLFretland, JGu, YHodous, BLHuang, XKim, JLLin, JLong, AMNguyen, HOlivieri, PRPatel, VFWang, LZhou, YHughes, PGeuns-Meyer, S Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase. Bioorg Med Chem Lett 19:424-7 (2008) [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:
BDBM14983
Synonyms:
4-Methyl-3-(3-(2-(methylamino)pyrimidin-4-yl)pyridin-2-yloxy)-N-(2-morpholino-5-(trifluoromethyl)phenyl)benzamide | 4-methyl-3-({3-[2-(methylamino)pyrimidin-4-yl]pyridin-2-yl}oxy)-N-[2-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]benzamide | CHEMBL219158 | pyridinyl pyrimidine 47
Type:
Small organic molecule
Emp. Form.:
C29H27F3N6O3
Mol. Mass.:
564.5583
SMILES:
CNc1nccc(n1)-c1cccnc1Oc1cc(ccc1C)C(=O)Nc1cc(ccc1N1CCOCC1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: