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Target
Angiopoietin-1 receptor
Ligand
BDBM50188749
Substrate
n/a
Meas. Tech.
ChEMBL_614510 (CHEMBL1111483)
IC50
259±n/a nM
Citation
 Morphy, R Selectively nonselective kinase inhibition: striking the right balance. J Med Chem 53:1413-37 (2010) [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:
BDBM50188749
Synonyms:
1-methyl-1-((5-(7-((4-methylpiperazin-1-yl)methyl)-1,4-dihydroindeno[1,2-c]pyrazol-3-yl)thiophen-2-yl)methyl)-3-(3-(trifluoromethyl)phenyl)urea | 1-methyl-1-((5-(7-((4-methylpiperazin-1-yl)methyl)-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)thiophen-2-yl)methyl)-3-(3-(trifluoromethyl)phenyl)urea | CHEMBL213910
Type:
Small organic molecule
Emp. Form.:
C30H31F3N6OS
Mol. Mass.:
580.667
SMILES:
CN(Cc1ccc(s1)-c1[nH]nc-2c1Cc1ccc(CN3CCN(C)CC3)cc-21)C(=O)Nc1cccc(c1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: