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Target
Prolyl endopeptidase FAP
Ligand
BDBM50171647
Substrate
n/a
Meas. Tech.
ChEMBL_321506 (CHEMBL880566)
IC50
4.6±n/a nM
Citation
 Hu, Y; Ma, L; Wu, M; Wong, MS; Li, B; Corral, S; Yu, Z; Nomanbhoy, T; Alemayehu, S; Fuller, SR; Rosenblum, JS; Rozenkrants, N; Minimo, LC; Ripka, WC; Szardenings, AK; Kozarich, JW; Shreder, KR Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7. Bioorg Med Chem Lett 15:4239-42 (2005) [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:
BDBM50171647
Synonyms:
CHEMBL373269 | N-alkyl Gly-boro-Pro derivative
Type:
Small organic molecule
Emp. Form.:
C16H27BN2O3
Mol. Mass.:
306.208
SMILES:
OB(O)[C@H]1CCCN1C(=O)CNC12CC3CC(CC(C3)C1)C2 |TLB:15:16:20:14.13.19,THB:17:18:13:16.21.15,17:16:13:18.20.19,15:14:20:16.21.17|
Structure:
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