| Assay ID | Title | Year | Journal | Article |
|---|
| AID1610455 | Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay | 2019 | Bioorganic & medicinal chemistry letters, 12-01, Volume: 29, Issue:23
| One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists. |
| AID364162 | Tmax in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1333365 | Induction of insulin secretion in ICR mouse primary pancreatic islets in presence of 16.8 mM glucose after 1 hr relative to control | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. |
| AID364164 | AUC in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364154 | Cmax in C57BL/6J mouse at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364152 | Inhibition of hERG upto 10 uM by patch clamp assay | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364149 | Agonist activity at mouse GPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364161 | Effect on glucose excursion in Sprague-Dawley rat at 30 mg/kg, po by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1688598 | Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells at 1 uM by firefly luciferase assay relative to AR231453 | | | |
| AID1732504 | Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes. |
| AID364168 | Inhibition of cytochrome | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1141038 | Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay relative to AR231453 | 2014 | Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
| Discovery of structurally novel, potent and orally efficacious GPR119 agonists. |
| AID364153 | Tmax in C57BL/6J mouse at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364147 | Agonist activity at CPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364157 | Agonist activity at GPR119 in hamster HIT-T15 cells stimulation of assessed as cAMP production | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364158 | Increase in glucose dependent insulin release in wild type C57BL/6J mouse at 20 mg/kg, po by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1333363 | Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. |
| AID364166 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364163 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1333366 | Induction of insulin secretion in ICR mouse primary pancreatic islets in presence of 2.8 mM glucose after 1 hr relative to control | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents. |
| AID364165 | Half life in Sprague-Dawley rat at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364159 | Increase in glucose dependent insulin release in GPR119 deficient C57BL/6J mouse at 20 mg/kg, po by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1141037 | Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay | 2014 | Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
| Discovery of structurally novel, potent and orally efficacious GPR119 agonists. |
| AID364160 | Increase in glucose dependent insulin release in diabetic KK/ay mouse by oral glucose tolerance test | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364167 | Activity at DPP4 | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364148 | Agonist activity at cynomolgus monkey GPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364156 | Half life in C57BL/6J mouse at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID645385 | Intrinsic activity at human GPR119 receptor assessed as cAMP production by HTRF assay relative to AR231453 | 2012 | Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
| Discovery of a second generation agonist of the orphan G-protein coupled receptor GPR119 with an improved profile. |
| AID364155 | AUC in C57BL/6J mouse at 10 mg/kg, po | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID596023 | Agonist activity at human GPR119 by melanophore assay | 2011 | Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
| Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. |
| AID364151 | Agonist activity at dog GPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID364150 | Agonist activity at rat GPR119 transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation | 2008 | Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
| Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. |
| AID1732505 | Agonist activity at human GPR119 stably transfected in CHO-K1 cells assessed as increase in cAMP stimulation after 1 hr by enzyme immunoassay relative to AR231453 | 2021 | Bioorganic & medicinal chemistry, 04-01, Volume: 35 | Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes. |
| AID1237202 | In vivo activation of GPR119 in normoglycemic 129SVE mouse assessed as increase in GIP level in plasma at 30 mg/kg, po measured after 45 mins relative to vehicle-treated control | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
| Discovery of a novel trans-1,4-dioxycyclohexane GPR119 agonist series. |
| AID1688599 | Agonist activity at CREB-LBD and Gal4-DBD fused recombinant human GPR119 expressed in HEK293 cells by firefly luciferase assay | | | |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1345261 | Human GPR119 (GPR18, GPR55 and GPR119) | 2007 | Endocrinology, Jun, Volume: 148, Issue:6
| A role for beta-cell-expressed G protein-coupled receptor 119 in glycemic control by enhancing glucose-dependent insulin release. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |