| Assay ID | Title | Year | Journal | Article |
|---|
| AID1511182 | Oral bioavailability in Sprague-Dawley rat at 5 mg/kg measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511176 | Inhibition of DGAT1 in mouse C2C12 cells assessed as reduction in intracellular triglyceride production incubated for 2 hrs in presence of BSA-complexed oleate by LC/MS/MS analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1889795 | Inhibition of human DGAT1 in serum starved HEK293 cells assessed as inhibition of triglyceride synthesis incubated for 20 mins followed by 13C-addition of 13C-oleic acid pre-complexed with BSA for 120 mins by LC-MS-based mass spectrophotometric analysis | 2022 | Bioorganic & medicinal chemistry letters, 04-15, Volume: 62 | Design and synthesis of novel spirocyclic carboxylic acids as potent and orally bioavailable DGAT1 inhibitors and their biological evaluation. |
| AID1511170 | Dissociation constant, pKa of compound | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511175 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1461869 | Reduction of olive oil-induced acute high-serum triglyceride level in C57/KSJ mouse at 1 to 10 mg/kg,po pretreated for 2 hrs followed by olive oil challenge post dose | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
| Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety. |
| AID1511177 | Antihyperlipidemic activity in Sprague-Dawley rat lipid bolus model assessed as reduction in plasma triglyceride excursion at 5 mg/kg, po administered via gavage 4 hrs prior to lipid challenge and measured upto 8 hrs post compound dose by GPO-Trinder meth | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511158 | Photo irritation factor, ratio of IC50 for cytotoxicity against BALB/c mouse 3T3 cells pretreated for 1 hr prior to 50 mins incubation in dark conditions followed by further incubation in DMEM medium for 20 to 22 hrs to IC50 for cytotoxicity against BALB/ | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511167 | Lipophilicity, log D of the compound at pH 7.4 | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511172 | Permeability across basolateral to apical side in human Caco2 cells | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511169 | Effective permeability coefficient, logPe of compound by PAMPA assay | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511188 | Half life in po dosed human plasma administered as single dose | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511173 | Efflux ratio of permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1461868 | Reduction in oleic acid-induced triglyceride generation in human HepG2 cells preincubated for 2 hrs followed oleic acid addition measured after 48 hrs by Oil Red O staining-based assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
| Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety. |
| AID1511181 | Tmax in Sprague-Dawley rat at 5 mg/kg, po measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511180 | Cmax in Sprague-Dawley rat at 5 mg/kg, po measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511179 | AUC (0 to 24 hrs) in Sprague-Dawley rat at 5 mg/kg, po measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511166 | Clearance in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511168 | Solubility of compound at pH 6.8 | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511174 | Protein binding in rat plasma | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511189 | Toxicity in human assessed as GI tolerability | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511159 | Inhibition of recombinant human his-tagged DGAT1 expressed in Sf9 insect cells using oleoyl-CoA and diolein as substrates incubated for 30 mins by LC/MS/MS analysis | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1511165 | Volume of distribution in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1169963 | Reduction in fasting triglyceride levels in familial chylomicronemia syndrome patient at 20 mg dosed daily | 2014 | ACS medicinal chemistry letters, Oct-09, Volume: 5, Issue:10
| Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety. |
| AID1062221 | Reduction in triglycerides in familial chylomicronemia syndrome patients measured after 3 weeks of compound dosing | 2013 | Journal of medicinal chemistry, Dec-27, Volume: 56, Issue:24
| Current status of the research and development of diacylglycerol O-acyltransferase 1 (DGAT1) inhibitors. |
| AID1511171 | Permeability across apical to basolateral side in human Caco2 cells | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1461867 | Reduction in oleic acid-induced triglyceride generation in human Caco-2 cells preincubated for 2 hrs followed oleic acid addition measured after 48 hrs by Oil Red O staining-based assay | 2017 | Bioorganic & medicinal chemistry, 09-01, Volume: 25, Issue:17
| Discovery of a low-systemic-exposure DGAT-1 inhibitor with a picolinoylpyrrolidine-2-carboxylic acid moiety. |
| AID1511163 | Half life in Sprague-Dawley rat at 1 mg/kg, iv measured upto 24 hrs | 2019 | ACS medicinal chemistry letters, Aug-08, Volume: 10, Issue:8
| Successful Strategies for Mitigation of a Preclinical Signal for Phototoxicity in a DGAT1 Inhibitor. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
| AID1347167 | Vero cells viability 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. |
| AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
| AID1347149 | Furin counterscreen 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. |
| 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. |
| 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. |
| 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. |
| AID1347153 | Confirmatory screen GU AMC 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. |
| AID1347156 | DAPI mCherry counterscreen 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. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7
| High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347168 | HepG2 cells viability 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. |
| 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| AID1347161 | Confirmatory 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. |
| AID1347152 | Confirmatory screen NINDS AMC 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. |
| AID1347158 | ZIKV-mCherry secondary 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. |
| AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
| AID1347172 | Secondary qRT-PCR qHTS assay for selected 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. |
| AID1347171 | Orthogonal mCherry assay for qRT-PCR qHTS of selected 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. |
| AID1347170 | Vero cells viability counterscreen for qRT-PCR qHTS assay of selected 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] |