| Assay ID | Title | Year | Journal | Article |
|---|
| AID1169046 | Volume of distribution in Beagle dog at 1 mg/kg, iv or 3 mg/kg, po | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169059 | Inhibition of CaCl2-induced abdominal aortic aneurysm in 129SvEv mouse assessed as reduction in aortic diameter at 1 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169053 | Drug metabolism in human liver microsomes after 30 mins at 4 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169037 | Inhibition of mouse cathepsin S using benzyloxycarbonyl-L-Leucyl-L-Arginine 4-Methyl-coumaryl-7-amide substrate by FRET assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169055 | Displacement of [3H]astemizole form human ERG expressed in HEK293 cell membranes at 100 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169063 | AUC (0 to 24 hrs) in 129SvEv mouse model of CaCl2-induced abdominal aortic aneurysm at 1 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169051 | Drug metabolism in rat liver microsomes after 30 mins at 4 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169048 | Inhibition of CYP2D6 (unknown origin) using bufuralol substrate at 10 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169057 | Stability in rat plasma assessed as loss of parent compound after 30 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169045 | Clearance in Beagle dog at 1 mg/kg, iv or 3 mg/kg, po | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169054 | Permeability from apical to basolateral side in MDCK cells at 2.5 uM incubated for 1 hr | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169042 | Dissociation constant, basic pKa of the compound | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169064 | AUC (0 to 24 hrs) in 129SvEv mouse model of CaCl2-induced abdominal aortic aneurysm at 3 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169036 | Inhibition of human cathepsin S using benzyloxycarbonyl-L-Leucyl-L-Arginine 4-Methyl-coumaryl-7-amide substrate by FRET assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169049 | Inhibition of CYP2C9 (unknown origin) using diclofenac substrate at 10 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169066 | AUC (0 to 24 hrs) in 129SvEv mouse model of CaCl2-induced abdominal aortic aneurysm at 30 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169041 | Lipophilicity, log D of the compound at pH 4.0 | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169040 | Lipophilicity, log P of the compound | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169047 | Inhibition of CYP3A4 (unknown origin) using midazolam substrate at 10 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169044 | Oral bioavailability in Beagle dog at 3 mg/kg | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169043 | Solubility in simulated gastric fluid | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169058 | Inhibition of CaCl2-induced abdominal aortic aneurysm in 129SvEv mouse assessed as reduction in aortic diameter at 1 to 30 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169052 | Drug metabolism in dog liver microsomes after 30 mins at 4 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169065 | AUC (0 to 24 hrs) in 129SvEv mouse model of CaCl2-induced abdominal aortic aneurysm at 10 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169056 | Stability in human plasma assessed as loss of parent compound after 30 mins | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169060 | Inhibition of CaCl2-induced abdominal aortic aneurysm in 129SvEv mouse assessed as reduction in aortic diameter at 3 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169050 | Drug metabolism in mouse liver microsomes after 30 mins at 4 uM | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169062 | Inhibition of CaCl2-induced abdominal aortic aneurysm in 129SvEv mouse assessed as reduction in aortic diameter at 30 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169061 | Inhibition of CaCl2-induced abdominal aortic aneurysm in 129SvEv mouse assessed as reduction in aortic diameter at 10 mg/kg dosed through oral gavage BID for 4 weeks with first dose given one day prior to surgery | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1169038 | Inhibition of rat cathepsin S G137C mutant using benzyloxycarbonyl-L-Leucyl-L-Arginine 4-Methyl-coumaryl-7-amide substrate by FRET assay | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |