Target
Prolyl endopeptidase FAP
Ligand
BDBM609535
Substrate
n/a
Meas. Tech.
In Vitro Assay Dipeptidyl Peptidase IV. Fibroblast Activation Protein and Prolyl Oligopeptidase
IC50
1.60±n/a nM
Citation
 Bachovchin, WWLai, HWu, W FAP-targeted radiopharmaceuticals and imaging agents, and uses related thereto US Patent  US11707539 Publication Date 7/25/2023
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:
BDBM609535
Synonyms:
DOTA-PABA-D- Ala-boroPro | US11707539, Compound 6572
Type:
Small organic molecule
Emp. Form.:
C30H46BN7O11
Mol. Mass.:
691.538
SMILES:
C[C@@H](NC(=O)c1ccc(NC(=O)CN2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)cc1)C(=O)N1CCC[C@H]1B(O)O |r|
Structure:
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