Target
Prolyl endopeptidase FAP
Ligand
BDBM50382283
Substrate
n/a
Meas. Tech.
Enzymatic Assay
pH
8.3±n/a
Temperature
310.15±n/a K
IC50
110±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:
BDBM50382283
Synonyms:
CHEMBL2022530 | US9346814, Ref. Cmpd No 1 (Example 2)
Type:
Small organic molecule
Emp. Form.:
C18H15F2N3O2
Mol. Mass.:
343.3274
SMILES:
FC1(F)C[C@@H](C#N)N(C1)C(=O)CNC(=O)c1cccc2ccccc12 |r|
Structure:
Search PDB for entries with ligand similarity: