CHEMBL1086968
Stopped at phase one || POP Ki 1.5 nM
General
Type : Peptide, Thiazolidine, Cyclopropyl, Indole, Sulfur Compound
Chemical_Nomenclature : [(2S,3aS,7aS)-2-(1,3-thiazolidine-3-carbonyl)-2,3,3a,4,5,6,7,7a-octahydroindol-1-yl]-[(1R,2R)-2-phenylcyclopropyl]methanone
Canonical SMILES : C1CCC2C(C1)CC(N2C(=O)C3CC3C4=CC=CC=C4)C(=O)N5CCSC5
InChI : InChI=1S\/C22H28N2O2S\/c25-21(18-13-17(18)15-6-2-1-3-7-15)24-19-9-5-4-8-16(19)12-20(24)22(26)23-10-11-27-14-23\/h1-3,6-7,16-20H,4-5,8-14H2\/t16-,17-,18+,19-,20-\/m0\/s1
InChIKey : NXSXRIHXEQSYEZ-KNJMJIDISA-N
Other name(s) : S 17092 || S-17092 || S17092 || SCHEMBL194654 || GTPL6565 || ZINC3825778 || S 17092-1
MW : 384.53
Formula : C22H28N2O2S
CAS_number : 176797-26-5
PubChem : 9929984
UniChem : NXSXRIHXEQSYEZ-KNJMJIDISA-N
IUPHAR : 6565
Target
Families : CHEMBL1086968 ligand of proteins in family
S9N_PPCE_Peptidase_S9
Protein :
human-PREP
References (12)
| Title : Computer-Aided Drug Discovery Identifies Alkaloid Inhibitors of Parkinson's Disease Associated Protein, Prolyl Oligopeptidase - Kulkarni_2021_Evid.Based.Complement.Alternat.Med_2021_6687572 |
| Author(s) : Kulkarni AM , Rampogu S , Lee KW |
| Ref : Evid Based Complement Alternat Med , 2021 :6687572 , 2021 |
| Abstract : |
| PubMedSearch : Kulkarni_2021_Evid.Based.Complement.Alternat.Med_2021_6687572 |
| PubMedID: 33897801 |
| Gene_locus related to this paper: human-PREP |
| Title : Hypothalamic prolyl endopeptidase (PREP) regulates pancreatic insulin and glucagon secretion in mice - Kim_2014_Proc.Natl.Acad.Sci.U.S.A_111_11876 |
| Author(s) : Kim JD , Toda C , D'Agostino G , Zeiss CJ , DiLeone RJ , Elsworth JD , Kibbey RG , Chan O , Harvey BK , Richie CT , Savolainen M , Myohanen T , Jeong JK , Diano S |
| Ref : Proc Natl Acad Sci U S A , 111 :11876 , 2014 |
| Abstract : |
| PubMedSearch : Kim_2014_Proc.Natl.Acad.Sci.U.S.A_111_11876 |
| PubMedID: 25071172 |
| Gene_locus related to this paper: human-PREP , mouse-ppce |
| Title : Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors - |
| Author(s) : Lawandi J , Gerber-Lemaire S , Juillerat-Jeanneret L , Moitessier N |
| Ref : Journal of Medicinal Chemistry , 53 :3423 , 2010 |
| PubMedID: 20058865 |
| Title : Psychotropic profile of S 17092, a prolyl endopeptidase inhibitor, using quantitative EEG in young healthy volunteers - Morain_2007_Neuropsychobiology_55_176 |
| Author(s) : Morain P , Boeijinga PH , Demazieres A , De Nanteuil G , Luthringer R |
| Ref : Neuropsychobiology , 55 :176 , 2007 |
| Abstract : |
| PubMedSearch : Morain_2007_Neuropsychobiology_55_176 |
| PubMedID: 17700042 |
| Title : Effect of prolyl endopeptidase inhibition on arginine-vasopressin and thyrotrophin-releasing hormone catabolism in the rat brain - Bellemere_2005_J.Neuroendocrinol_17_306 |
| Author(s) : Bellemere G , Vaudry H , Morain P , Jegou S |
| Ref : J Neuroendocrinol , 17 :306 , 2005 |
| Abstract : |
| PubMedSearch : Bellemere_2005_J.Neuroendocrinol_17_306 |
| PubMedID: 15869566 |
| Title : Prolyl oligopeptidase is involved in release of the antifibrotic peptide Ac-SDKP - Cavasin_2004_Hypertension_43_1140 |
| Author(s) : Cavasin MA , Rhaleb NE , Yang XP , Carretero OA |
| Ref : Hypertension , 43 :1140 , 2004 |
| Abstract : |
| PubMedSearch : Cavasin_2004_Hypertension_43_1140 |
| PubMedID: 15037553 |
| Gene_locus related to this paper: human-PREP |
| Title : Effect of S 17092, a novel prolyl endopeptidase inhibitor, on substance P and alpha-melanocyte-stimulating hormone breakdown in the rat brain - Bellemere_2003_J.Neurochem_84_919 |
| Author(s) : Bellemere G , Morain P , Vaudry H , Jegou S |
| Ref : Journal of Neurochemistry , 84 :919 , 2003 |
| Abstract : |
| PubMedSearch : Bellemere_2003_J.Neurochem_84_919 |
| PubMedID: 12603817 |
| Title : S 17092: a prolyl endopeptidase inhibitor as a potential therapeutic drug for memory impairment. Preclinical and clinical studies - Morain_2002_CNS.Drug.Rev_8_31 |
| Author(s) : Morain P , Lestage P , De Nanteuil G , Jochemsen R , Robin JL , Guez D , Boyer PA |
| Ref : CNS Drug Rev , 8 :31 , 2002 |
| Abstract : |
| PubMedSearch : Morain_2002_CNS.Drug.Rev_8_31 |
| PubMedID: 12070525 |
| Title : Effects of the prolyl endopeptidase inhibitor S 17092 on cognitive deficits in chronic low dose MPTP-treated monkeys - Schneider_2002_Neuropsychopharmacology_26_176 |
| Author(s) : Schneider JS , Giardiniere M , Morain P |
| Ref : Neuropsychopharmacology , 26 :176 , 2002 |
| Abstract : |
| PubMedSearch : Schneider_2002_Neuropsychopharmacology_26_176 |
| PubMedID: 11790513 |
| Title : Pharmacodynamic and pharmacokinetic profile of S 17092, a new orally active prolyl endopeptidase inhibitor, in elderly healthy volunteers. A phase I study - Morain_2000_Br.J.Clin.Pharmacol_50_350 |
| Author(s) : Morain P , Robin JL , De Nanteuil G , Jochemsen R , Heidet V , Guez D |
| Ref : British Journal of Clinical Pharmacology , 50 :350 , 2000 |
| Abstract : |
| PubMedSearch : Morain_2000_Br.J.Clin.Pharmacol_50_350 |
| PubMedID: 11012558 |
| Title : Novel proline endopeptidase inhibitors do not modify Abeta40\/42 formation and degradation by human cells expressing wild-type and swedish mutated beta-amyloid precursor protein - Petit_2000_Br.J.Pharmacol_130_1613 |
| Author(s) : Petit A , Barelli H , Morain P , Checler F |
| Ref : British Journal of Pharmacology , 130 :1613 , 2000 |
| Abstract : |
| PubMedSearch : Petit_2000_Br.J.Pharmacol_130_1613 |
| PubMedID: 10928965 |
| Title : S 17092-1, a highly potent, specific and cell permeant inhibitor of human proline endopeptidase - Barelli_1999_Biochem.Biophys.Res.Commun_257_657 |
| Author(s) : Barelli H , Petit A , Hirsch E , Wilk S , De Nanteuil G , Morain P , Checler F |
| Ref : Biochemical & Biophysical Research Communications , 257 :657 , 1999 |
| Abstract : |
| PubMedSearch : Barelli_1999_Biochem.Biophys.Res.Commun_257_657 |
| PubMedID: 10208839 |