Reaction Details Report a problem with these data
Target
Prolyl endopeptidase FAP
Ligand
BDBM50050521
Substrate
n/a
Meas. Tech.
In Vitro Inhibition Assay
IC50
29000±n/a nM
Citation
 Bachovchin, WW; Lai, H; Wu, W Combination therapies using immuno-dash inhibitors and PGE2 antagonists US Patent  US11096924 Publication Date 8/24/2021 
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:
BDBM50050521
Synonyms:
(2-Dihydroxyborane-pyrrolidin-1-yl)-pyrrolidin-2-yl-methanone(PBP) | (2R)-N-[(2R)-2-(DIHYDROXYBORYL)-1-L-PROLYLPYRROLIDIN-2-YL]-N-[(5R)-5-(DIHYDROXYBORYL)-1-L-PROLYLPYRROLIDIN-2-YL]-L-PROLINAMIDE | Boronic acid derivative | CHEMBL63895 | US11096924, DASH-inhibitors 1181 | US11559537, Compound 1181
Type:
Small organic molecule
Emp. Form.:
C9H17BN2O3
Mol. Mass.:
212.054
SMILES:
OB(O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1
Structure:
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