| Assay ID | Title | Year | Journal | Article |
|---|
| 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. |
| 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. |
| 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. |
| AID1820690 | Apparent volume of distribution in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID1820680 | Plasma protein binding in human plasma assessed as unbound fraction | | | |
| AID779564 | Selectivity ratio of human mu opioid receptor over human Cav 1.2 ion channel | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779578 | Inhibition of human Nav 1.5 tonic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820694 | Displacement of [3H]-Diprenorphine from human mu opiod receptor expressed in CHO cells incubated for 1 hr by competition binding assay | | | |
| AID779568 | Cardiotoxicity in isolated rabbit left ventricular wedge model assessed as proarrhyhmic event | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779582 | Analgesic effect in mouse by hot plate assay relative to morphine | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779581 | Analgesic effect in rat by hot plate assay relative to morphine | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820703 | Drug concentration in Sprague-Dawley rat brain at 0.25 mg/kg, iv measured after 5 mins by LC-MS/MS analysis | | | |
| AID1820686 | Inhibition of human ERG expressed in CHO cells at holding potential of -80 mV by whole cell patch clamp assay | | | |
| AID779575 | Cardiotoxicity in isolated rabbit left ventricular wedge model assessed as increase in QT interval at 0.3 uM | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779596 | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779566 | Selectivity ratio of human mu opioid receptor over human ERG channel | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820685 | Inhibition of CYP2C19 (unknown origin) | | | |
| AID1820679 | Metabolic stability in dog liver microsomes assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis | | | |
| AID779569 | Cardiotoxicity in cynomolgus monkey assessed as QT interval | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779584 | Selectivity ratio of EC50 for human mu opioid receptor expressed in HEK293 cells over EC50 for human kappa opioid receptor expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820682 | Plasma protein binding in dog plasma assessed as unbound fraction | | | |
| AID779565 | Selectivity ratio of human mu opioid receptor over human Nav 1.5 tonic ion channel | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820684 | Inhibition of CYP2C9 (unknown origin) | | | |
| AID1820691 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID779586 | Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820678 | Agonist activity at mu opioid receptor (unknown origin) assessed as maximal cAMP level incubated for 40 mins by spectrophotometry relative to DAMGO | | | |
| AID1820706 | Agonist activity at mu opioid receptor (unknown origin) assessed as beta arrestin-2 recruitment incubated for 3 days by PathHunter assay | | | |
| AID1820692 | Half life in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID1820697 | Agonist activity at human kappa opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | | | |
| AID779567 | Selectivity ratio of human mu opioid receptor over human Nav 1.5 phasic ion channel | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779595 | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay relative to morphine | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779585 | Agonist activity at human delta opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820689 | AUC(0 to infinity) in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID779593 | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay relative to morphine | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779574 | Cardiotoxicity in isolated rabbit left ventricular wedge model assessed as increase in Tp-e interval at 1 uM | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779580 | Inhibition of human ERG channel expressed in HEK293 cells by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820676 | Apparent permeability across apical to basal membrane in human Caco-2 cells | | | |
| AID779572 | Cardiotoxicity in cynomolgus monkey assessed as QRS duration | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820708 | Toxicity in Sprague-Dawley rat assessed as effect on blood oxygen levels at 1.56 mg/kg, sc measured after 30 mins by blood gas analyzer | | | |
| AID1820674 | Efflux ratio of permeability in human Caco-2 cells | | | |
| AID1820699 | Antinociceptive activity in Sprague-Dawley rat assessed as increase in paw withdrawal latency at 1 mg/kg, sc measured after 30 mins by Hot-plate test | | | |
| AID779594 | Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779577 | Inhibition of human Cav 1.2 ion channel expressed in HEK293 cells by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820677 | Metabolic stability in human liver microsomes assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis | | | |
| AID1820681 | Plasma protein binding in rat plasma assessed as unbound fraction | | | |
| AID1820704 | Ratio of drug concentration in brain to plasma of Sprague-Dawley rat at 2 mg/kg, iv measured at 0.25 hrs by LC-MS/MS analysis | | | |
| AID1820673 | Agonist activity at mu opioid receptor (unknown origin) assessed as increase in cAMP level incubated for 40 mins by spectrophotometry | | | |
| AID1820696 | Agonist activity at human delta opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | | | |
| AID1820675 | Metabolic stability in rat liver microsomes assessed as intrinsic clearance preincubated for 10 mins followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis | | | |
| AID779579 | Inhibition of human Nav 1.5 phasic ion channel expressed in HEK293 cells by whole-cell patch clamp technique | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820710 | Half life of compound | | | |
| AID779583 | Selectivity ratio of EC50 for human mu opioid receptor expressed in HEK293 cells over EC50 for human delta opioid receptor expressed in HEK293 cells | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820693 | MRT in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID779562 | Cardiotoxicity in isolated rabbit left ventricular wedge model assessed as torsade de pointes score up to 30 uM | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779576 | Binding affinity to human mu opioid receptor by radio-ligand binding assay | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID779571 | Cardiotoxicity in cynomolgus monkey assessed as PR interval | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820683 | Inhibition of CYP1A2 (unknown origin) | | | |
| AID1820695 | Agonist activity at human mu opioid receptor expressed in HEK293 assessed as increase in calcium mobilization incubated for 60 mins by FLIPR assay | | | |
| AID1820688 | AUClast in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| AID1820707 | Agonist activity at mu opioid receptor (unknown origin) assessed as maximal beta arrestin-2 recruitment incubated for 3 days by PathHunter assay relative to DAMGO | | | |
| AID1820700 | Antinociceptive activity in sc dosed Sprague-Dawley rat assessed as increase in thermal pain threshold measured after 30 mins by Hot-plate test | | | |
| AID1820705 | Drug concentration in Sprague-Dawley rat liver at 0.25 mg/kg,iv measured after 30 mins by LC-MS/MS analysis | | | |
| AID779570 | Cardiotoxicity in cynomolgus monkey assessed as QTc interval | 2013 | Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20
| Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. |
| AID1820687 | Cmax in Sprague-Dawley rat at 2 mg/kg, iv by LC-MS/MS analysis | | | |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |