Target
Prolyl endopeptidase FAP
Ligand
BDBM50434169
Substrate
n/a
Meas. Tech.
ChEMBL_1335495 (CHEMBL3239280)
IC50
11±n/a nM
Citation
 Jansen, KHeirbaut, LVerkerk, RCheng, JDJoossens, JCos, PMaes, LLambeir, AMDe Meester, IAugustyns, KVan der Veken, P Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). J Med Chem 57:3053-74 (2014) [PubMed]  Article 
Target
Name:
Prolyl endopeptidase FAP
Synonyms:
Fap | Fibroblast activation protein (FAP) | SEPR_MOUSE | Seprase
Type:
Enzyme
Mol. Mass.:
87949.14
Organism:
Mouse
Description:
P97321
Residue:
761
Sequence:
MKTWLKTVFGVTTLAALALVVICIVLRPSRVYKPEGNTKRALTLKDILNGTFSYKTYFPNWISEQEYLHQSEDDNIVFYNIETRESYIILSNSTMKSVNATDYGLSPDRQFVYLESDYSKLWRYSYTATYYIYDLQNGEFVRGYELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPGDPPFQITYTGRENRIFNGIPDWVYEEEMLATKYALWWSPDGKFLAYVEFNDSDIPIIAYSYYGDGQYPRTINIPYPKAGAKNPVVRVFIVDTTYPHHVGPMEVPVPEMIASSDYYFSWLTWVSSERVCLQWLKRVQNVSVLSICDFREDWHAWECPKNQEHVEESRTGWAGGFFVSTPAFSQDATSYYKIFSDKDGYKHIHYIKDTVENAIQITSGKWEAIYIFRVTQDSLFYSSNEFEGYPGRRNIYRISIGNSPPSKKCVTCHLRKERCQYYTASFSYKAKYYALVCYGPGLPISTLHDGRTDQEIQVLEENKELENSLRNIQLPKVEIKKLKDGGLTFWYKMILPPQFDRSKKYPLLIQVYGGPCSQSVKSVFAVNWITYLASKEGIVIALVDGRGTAFQGDKFLHAVYRKLGVYEVEDQLTAVRKFIEMGFIDEERIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASIYSERFMGLPTKDDNLEHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNAQVDFQAMWYSDQNHGISSGRSQNHLYTHMTHFLKQCFSLSD
  
Inhibitor
Name:
BDBM50434169
Synonyms:
CHEMBL2385300 | US9346814, Cmpd No 22 Example 26
Type:
Small organic molecule
Emp. Form.:
C17H15BrN4O2
Mol. Mass.:
387.231
SMILES:
Brc1cccc2nccc(C(=O)NCC(=O)N3CCC[C@H]3C#N)c12 |r|
Structure:
Search PDB for entries with ligand similarity: