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Target
Prolyl endopeptidase FAP
Ligand
BDBM50134186
Substrate
n/a
Meas. Tech.
ChEMBL_1537821 (CHEMBL3737792)
IC50
22000±n/a nM
Citation
 Chen, P; Feng, D; Qian, X; Apgar, J; Wilkening, R; Kuethe, JT; Gao, YD; Scapin, G; Cox, J; Doss, G; Eiermann, G; He, H; Li, X; Lyons, KA; Metzger, J; Petrov, A; Wu, JK; Xu, S; Weber, AE; Yan, Y; Roy, RS; Biftu, T Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin. Bioorg Med Chem Lett 25:5767-71 (2015) [PubMed]  Article 
Target
Name:
Prolyl endopeptidase FAP
Synonyms:
APCE | Antiplasmin-cleaving enzyme FAP, soluble form | Dipeptidyl peptidase FAP | FAP | FAPalpha | Fibroblast activation protein alpha | Gelatine degradation protease FAP | Integral membrane serine protease | Post-proline cleaving enzyme | Prolyl endopeptidase FAP | SEPR_BOVIN | SIMP | Seprase | Serine integral membrane protease | Surface-expressed protease | Z-Pro-prolinal insensitive peptidase | ZIP
Type:
PROTEIN
Mol. Mass.:
87742.67
Organism:
Bos taurus
Description:
ChEMBL_116681
Residue:
760
Sequence:
MKTWLKIVFGVATSAVLALLVMCIVLRPSRVHNSEESTTRALTLKDILNGTFSYKTFFPNWISGQEYLHQSTDNNVVFYNIETGESYTILSNTTMKSVNASNYGLSPDRQFAYLESDYSKLWRYSYTATYHIYDLTNGEFIRRNELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPEDPPFQITYNGKENKIFNGIPDWVYEEEMLATKYALWWSPNGKFLAYAEFNDTEIPVIAYSYYGDEQYPRTINIPYPKAGAKNPVVRIFIIDATYPEHIGPREVPVPAMIASSDYYFSWLTWVTDDRICLQWLKRIQNVSVLSTCDFREDWQTWNCPKTQEHIEESRTGWAGGFFVSTPVFSHDTISYYKIFSDKDGYKHIHYIRDTVENAIQITSGKWEAINIFRVTQDSLFYSSNEFEGYPGRRNIYRISIGSHSPSKKCITCHLRKKRCQYYTASFSDYAKYYALVCYGPGLPISTLHDGRTDQEIKILEDNKELENALKNIQLPKEEIKKLKVDDITLWYKMILPPQFDKSKKYPLLIQVYGGPCSQSVRSIFAVSWISYLASKEGIVIALVDGRGTAFQGDKLLYAVYRKLGVYEVEDQITAVRKFIEMGFIDEKRIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASIYTERFMGLPTKDDNLKHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNAQVDFQAMWYSDQNHGLSGLSTKHLYTHMTHFLKQCFSLSD
  
Inhibitor
Name:
BDBM50134186
Synonyms:
CHEMBL3734964
Type:
Small organic molecule
Emp. Form.:
C20H23F2N5O2
Mol. Mass.:
403.4257
SMILES:
N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2[nH]nc(NC(=O)C3CC3)c2C1 |r|
Structure:
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