Assay ID | Title | Year | Journal | Article |
AID1280006 | Oral bioavailability in dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280005 | Oral bioavailability in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID765089 | Binding affinity to orexin receptor 1 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
| Selective orexin receptor antagonists. |
AID1279994 | Binding affinity to OX1R (unknown origin) | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1279956 | Effect on sleep parameter in po dosed rat by EEG analysis | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID765090 | Binding affinity to orexin receptor 2 (unknown origin) | 2013 | Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
| Selective orexin receptor antagonists. |
AID1190414 | Antagonist activity at human OX2R by radioligand displacement assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant. |
AID1280007 | Effect on sleep parameter in po dosed dog by EEG analysis | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280001 | Clearance in iv dosed rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280000 | Receptor occupancy at OX2R in rat brain assessed as drug level in plasma | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1190417 | Antagonist activity at human OX1R by FLIPR assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant. |
AID1190415 | Antagonist activity at human OX1R by radioligand displacement assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant. |
AID1237021 | Antagonist activity at orexin-2 receptor (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
| Recent trends in orexin research--2010 to 2015. |
AID1280008 | Antagonist activity at human OX2R expressed in CHO cell membranes assessed as inhibition of orexin-A-induced intracellular calcium release after 120 mins | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1237020 | Antagonist activity at orexin-1 receptor (unknown origin) | 2015 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
| Recent trends in orexin research--2010 to 2015. |
AID1582240 | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. |
AID1280003 | Clearance in iv dosed dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1582239 | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liqu | 2020 | Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
| Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis. |
AID1279997 | Plasma protein binding in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1190418 | Selectivity ratio of Ki for human OX1R to Ki for human OX2R | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant. |
AID1280009 | Ratio of drug level in CSF to plasma in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1279957 | Antagonist activity at human OX1R expressed in CHO cell membranes assessed as inhibition of orexin-A-induced intracellular calcium release after 120 mins | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1190416 | Antagonist activity at human OX2R by FLIPR assay | 2015 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 25, Issue:3
| Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant. |
AID1279986 | Plasma protein binding in human | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280002 | Half life in iv dosed rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280004 | Half life in iv dosed dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1279993 | Binding affinity to OX2R (unknown origin) | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1280010 | Ratio of drug level in brain to plasma in rat | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
AID1279998 | Plasma protein binding in dog | 2016 | Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2
| Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. |
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. |
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. |
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. |
AID1346418 | Human OX2 receptor (Orexin receptors) | 2012 | Neuropharmacology, Feb, Volume: 62, Issue:2
| Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. |
AID1346381 | Human OX1 receptor (Orexin receptors) | 2012 | Neuropharmacology, Feb, Volume: 62, Issue:2
| Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |