Reaction Details |
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Target | Prolyl endopeptidase FAP |
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Ligand | BDBM50173973 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_328425 (CHEMBL863966) |
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Ki | 7925±n/a nM |
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Citation | Haffner, CD; McDougald, DL; Reister, SM; Thompson, BD; Conlee, C; Fang, J; Bass, J; Lenhard, JM; Croom, D; Secosky-Chang, MB; Tomaszek, T; McConn, D; Wells-Knecht, K; Johnson, PR 2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV. Bioorg Med Chem Lett15:5257-61 (2005) [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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BDBM50173973 |
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n/a |
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Name | BDBM50173973 |
Synonyms: | CHEMBL201053 | N-(4-(((R)-3-amino-4-((2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl)-2-methyl-4-oxobutan-2-ylsulfonyl)methyl)phenyl)acetamide |
Type | Small organic molecule |
Emp. Form. | C19H25FN4O4S |
Mol. Mass. | 424.49 |
SMILES | CC(=O)Nc1ccc(CS(=O)(=O)C(C)(C)[C@H](N)C(=O)N2C[C@@H](F)C[C@H]2C#N)cc1 |
Structure |
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