Target
Prolyl endopeptidase FAP
Ligand
BDBM50434166
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
8.3±n/a
Temperature
310.15±n/a K
IC50
10.3±0.7 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:
BDBM50434166
Synonyms:
CHEMBL2385270 | US9346814, Cmpd No 6 Example 9
Type:
Small organic molecule
Emp. Form.:
C17H15FN4O2
Mol. Mass.:
326.325
SMILES:
Fc1ccc2nccc(C(=O)NCC(=O)N3CCC[C@H]3C#N)c2c1 |r|
Structure:
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