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Target
Angiopoietin-1 receptor
Ligand
BDBM50145570
Substrate
n/a
Meas. Tech.
ChEBML_210883
IC50
520±n/a nM
Citation
 Borhani, DW; Calderwood, DJ; Friedman, MM; Hirst, GC; Li, B; Leung, AK; McRae, B; Ratnofsky, S; Ritter, K; Waegell, W A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. Bioorg Med Chem Lett 14:2613-6 (2004) [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:
BDBM50145570
Synonyms:
1H-Indole-2-carboxylic acid (4-{4-amino-1-[4-(4-methyl-piperazin-1-yl)-cyclohexyl]-1H-pyrazolo[3,4-d]pyrimidin-3-yl}-2-methoxy-phenyl)-amide | CHEMBL431609
Type:
Small organic molecule
Emp. Form.:
C32H37N9O2
Mol. Mass.:
579.6953
SMILES:
COc1cc(ccc1NC(=O)c1cc2ccccc2[nH]1)-c1nn([C@H]2CC[C@@H](CC2)N2CCN(C)CC2)c2ncnc(N)c12 |wU:23.25,wD:26.32,(1.45,-1.92,;1.52,-3.48,;2.9,-4.2,;2.97,-5.74,;4.32,-6.46,;5.63,-5.64,;5.57,-4.09,;4.21,-3.37,;4.2,-1.83,;5.51,-1.03,;6.86,-1.8,;5.49,.51,;6.63,1.55,;5.98,2.93,;6.61,4.35,;5.7,5.59,;4.18,5.43,;3.55,4.03,;4.46,2.77,;4.16,1.25,;4.39,-8,;5.62,-8.89,;5.14,-10.36,;6.09,-11.55,;7.63,-11.32,;8.58,-12.52,;8.02,-13.95,;6.49,-14.19,;5.53,-12.99,;8.99,-15.14,;10.5,-14.91,;11.47,-16.1,;10.91,-17.54,;11.88,-18.76,;9.38,-17.78,;8.43,-16.58,;3.61,-10.36,;2.57,-11.5,;1.08,-11.17,;.61,-9.71,;1.64,-8.57,;1.17,-7.1,;3.13,-8.89,)|
Structure:
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