Target
Prolyl endopeptidase FAP
Ligand
BDBM50434159
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
8.3±n/a
Temperature
310.15±n/a K
IC50
420±40 nM
Comments
extracted
Citation
 Jansen, KDe Meester, IHeirbaut, LCheng, JDJoossens, JAugustyns, KVan Der Veken, P FAP inhibitors US Patent  US9346814 Publication Date 5/24/2016
Target
Name:
Prolyl endopeptidase FAP
Synonyms:
Fap | Fibroblast activation protein (FAP) | SEPR_MOUSE | Seprase
Type:
Enzyme
Mol. Mass.:
87949.14
Organism:
Mus musculus (Mouse)
Description:
P97321
Residue:
761
Sequence:
MKTWLKTVFGVTTLAALALVVICIVLRPSRVYKPEGNTKRALTLKDILNGTFSYKTYFPNWISEQEYLHQSEDDNIVFYNIETRESYIILSNSTMKSVNATDYGLSPDRQFVYLESDYSKLWRYSYTATYYIYDLQNGEFVRGYELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPGDPPFQITYTGRENRIFNGIPDWVYEEEMLATKYALWWSPDGKFLAYVEFNDSDIPIIAYSYYGDGQYPRTINIPYPKAGAKNPVVRVFIVDTTYPHHVGPMEVPVPEMIASSDYYFSWLTWVSSERVCLQWLKRVQNVSVLSICDFREDWHAWECPKNQEHVEESRTGWAGGFFVSTPAFSQDATSYYKIFSDKDGYKHIHYIKDTVENAIQITSGKWEAIYIFRVTQDSLFYSSNEFEGYPGRRNIYRISIGNSPPSKKCVTCHLRKERCQYYTASFSYKAKYYALVCYGPGLPISTLHDGRTDQEIQVLEENKELENSLRNIQLPKVEIKKLKDGGLTFWYKMILPPQFDRSKKYPLLIQVYGGPCSQSVKSVFAVNWITYLASKEGIVIALVDGRGTAFQGDKFLHAVYRKLGVYEVEDQLTAVRKFIEMGFIDEERIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASIYSERFMGLPTKDDNLEHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNAQVDFQAMWYSDQNHGISSGRSQNHLYTHMTHFLKQCFSLSD
  
Inhibitor
Name:
BDBM50434159
Synonyms:
CHEMBL2385277 | US9346814, Ref Cmpd No 7 (example 17)
Type:
Small organic molecule
Emp. Form.:
C17H16N4O2
Mol. Mass.:
308.3345
SMILES:
O=C(CNC(=O)c1cccc2ncccc12)N1CCC[C@H]1C#N |r|
Structure:
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