Reaction Details Report a problem with these data
Target
Prolyl endopeptidase FAP
Ligand
BDBM12178
Substrate
BDBM11526
Meas. Tech.
Enzyme Inhibition Assay
IC50
175±n/a nM
Citation
Tsai, TY; Coumar, MS; Hsu, T; Hsieh, HP; Chien, CH; Chen, CT; Chang, CN; Lo, YK; Wu, SH; Huang, CY; Huang, YW; Wang, MH; Wu, HY; Lee, HJ; Chen, X; Chao, YS; Jiaang, WT Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors. Bioorg Med Chem Lett 16:3268-72 (2006) [PubMed] Article
More Info.:
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:
BDBM12178
Synonyms:
(2S)-1-{[(2S,4S)-4-(2,3-dihydro-1H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl}pyrrolidine-2-carbonitrile | pyrrolidine-2,4-dicarboxylic acid amide 11a
Type:
Small organic molecule
Emp. Form.:
C19H22N4O2
Mol. Mass.:
338.4036
SMILES:
O=C([C@@H]1CN[C@@H](C1)C(=O)N1CCC[C@H]1C#N)N1Cc2ccccc2C1 |r|