Reaction Details |
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Target | Prolyl endopeptidase FAP |
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Ligand | BDBM50338518 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_728477 (CHEMBL1685354) |
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Ki | >30000±n/a nM |
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Citation | Andrews, KM; Beebe, DA; Benbow, JW; Boyer, DA; Doran, SD; Hui, Y; Liu, S; McPherson, RK; Neagu, C; Parker, JC; Piotrowski, DW; Schneider, SR; Treadway, JL; VanVolkenberg, MA; Zembrowski, WJ 1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes. Bioorg Med Chem Lett21:1810-4 (2011) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Prolyl endopeptidase FAP |
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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: | MKTWVKIVFGVATSAVLALLVMCIVLRPSRVHNSEENTMRALTLKDILNGTFSYKTFFPN
WISGQEYLHQSADNNIVLYNIETGQSYTILSNRTMKSVNASNYGLSPDRQFVYLESDYSK
LWRYSYTATYYIYDLSNGEFVRGNELPRPIQYLCWSPVGSKLAYVYQNNIYLKQRPGDPP
FQITFNGRENKIFNGIPDWVYEEEMLATKYALWWSPNGKFLAYAEFNDTDIPVIAYSYYG
DEQYPRTINIPYPKAGAKNPVVRIFIIDTTYPAYVGPQEVPVPAMIASSDYYFSWLTWVT
DERVCLQWLKRVQNVSVLSICDFREDWQTWDCPKTQEHIEESRTGWAGGFFVSTPVFSYD
AISYYKIFSDKDGYKHIHYIKDTVENAIQITSGKWEAINIFRVTQDSLFYSSNEFEEYPG
RRNIYRISIGSYPPSKKCVTCHLRKERCQYYTASFSDYAKYYALVCYGPGIPISTLHDGR
TDQEIKILEENKELENALKNIQLPKEEIKKLEVDEITLWYKMILPPQFDRSKKYPLLIQV
YGGPCSQSVRSVFAVNWISYLASKEGMVIALVDGRGTAFQGDKLLYAVYRKLGVYEVEDQ
ITAVRKFIEMGFIDEKRIAIWGWSYGGYVSSLALASGTGLFKCGIAVAPVSSWEYYASVY
TERFMGLPTKDDNLEHYKNSTVMARAEYFRNVDYLLIHGTADDNVHFQNSAQIAKALVNA
QVDFQAMWYSDQNHGLSGLSTNHLYTHMTHFLKQCFSLSD
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BDBM50338518 |
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n/a |
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Name | BDBM50338518 |
Synonyms: | 1-((3S,4S)-4-amino-1-(4-(3,3-difluoropyrrolidin-1-yl)-1,3,5-triazin-2-yl)pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one | CHEMBL1683571 |
Type | Small organic molecule |
Emp. Form. | C16H21F4N7O |
Mol. Mass. | 403.3779 |
SMILES | N[C@H]1CN(C[C@@H]1N1CC(F)(F)CCC1=O)c1ncnc(n1)N1CCC(F)(F)C1 |r| |
Structure |
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