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Target
Prolyl endopeptidase FAP
Ligand
BDBM50248621
Substrate
n/a
Meas. Tech.
ChEMBL_541593 (CHEMBL1011682)
IC50
>20000±n/a nM
Citation
 Tsai, TY; Hsu, T; Chen, CT; Cheng, JH; Yeh, TK; Chen, X; Huang, CY; Chang, CN; Yeh, KC; Hsieh, SH; Chien, CH; Chang, YW; Huang, CH; Huang, YW; Huang, CL; Wu, SH; Wang, MH; Lu, CT; Chao, YS; Jiaang, WT Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors. Bioorg Med Chem 17:2388-99 (2009) [PubMed]  Article
Target
Name:
Prolyl endopeptidase FAP
Synonyms:
170 kDa melanoma membrane-bound gelatinase | FAP | Fibroblast Activation Protein (FAP) | Fibroblast activation protein alpha | Integral membrane serine protease | SEPR_HUMAN | Seprase
Type:
Enzyme
Mol. Mass.:
87712.48
Organism:
Homo sapiens (Human)
Description:
Q12884
Residue:
760
Sequence:
MKTWVKIVFGVATSAVLALLVMCIVLRPSRVHNSEENTMRALTLKDILNGTFSYKTFFPNWISGQEYLHQSADNNIVLYNIETGQSYTILSNRTMKSVNASNYGLSPDRQFVYLESDYSKLWRYSYTATYYIYDLSNGEFVRGNELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPGDPPFQITFNGRENKIFNGIPDWVYEEEMLATKYALWWSPNGKFLAYAEFNDTDIPVIAYSYYGDEQYPRTINIPYPKAGAKNPVVRIFIIDTTYPAYVGPQEVPVPAMIASSDYYFSWLTWVTDERVCLQWLKRVQNVSVLSICDFREDWQTWDCPKTQEHIEESRTGWAGGFFVSTPVFSYDAISYYKIFSDKDGYKHIHYIKDTVENAIQITSGKWEAINIFRVTQDSLFYSSNEFEEYPGRRNIYRISIGSYPPSKKCVTCHLRKERCQYYTASFSDYAKYYALVCYGPGIPISTLHDGRTDQEIKILEENKELENALKNIQLPKEEIKKLEVDEITLWYKMILPPQFDRSKKYPLLIQVYGGPCSQSVRSVFAVNWISYLASKEGMVIALVDGRGTAFQGDKLLYAVYRKLGVYEVEDQITAVRKFIEMGFIDEKRIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASVYTERFMGLPTKDDNLEHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNAQVDFQAMWYSDQNHGLSGLSTNHLYTHMTHFLKQCFSLSD
  
Inhibitor
Name:
BDBM50248621
Synonyms:
3-({2-[(2S,4S)-2-Cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl}amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide | CHEMBL517776
Type:
Small organic molecule
Emp. Form.:
C21H26ClFN4O2
Mol. Mass.:
420.908
SMILES:
CC(C)(CC(=O)N[C@H]1C[C@@H]1c1cccc(Cl)c1)NCC(=O)N1C[C@@H](F)C[C@H]1C#N |r|
Structure:
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