| Assay ID | Title | Year | Journal | Article |
|---|
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | | | |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
| AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1
| High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | | | |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7
| A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
| Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1275300 | Induction of gastric emptying rate in Sprague-Dawley rat at 5 mg/kg, iv administered prior to feeding along with cisplatin injection measured after 40 mins | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1892546 | Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID1900870 | Inhibition of hERG expressed in CHO-K1 cells assessed as inhibition of channel current at 1 uM by manual patch clamp method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | Discovery of novel verinurad analogs as dual inhibitors of URAT1 and GLUT9 with improved Druggability for the treatment of hyperuricemia. |
| AID1862594 | Inhibition of human ERG potassium channel expressed in CHO cells by automated patch clamp electrophysiological assay | | | |
| AID672174 | Selectivity ratio of Ki for human 5HT3A receptor to Ki for human 5HT4C receptor | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID1729992 | Inhibition of human ERG at 30 nM by patch clamp method relative to control | | | |
| AID1275305 | Tmax in rat at 5 mg/kg, po | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1824585 | Inhibition of hERG expressed in CHO cells at -80 mV holding potential by automated patch clamp method | 2022 | European journal of medicinal chemistry, Feb-05, Volume: 229 | The novel therapeutic strategy of vilazodone-donepezil chimeras as potent triple-target ligands for the potential treatment of Alzheimer's disease with comorbid depression. |
| AID1275307 | AUCinfinity in rat at 5 mg/kg, po | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1892538 | Antiproliferative activity against human A2780/CDDP cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID683467 | Induction of 5HT4-receptor mediated esophagal relaxation in iv dosed Sprague-Dawley rat | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID1520478 | Inhibition of human ERG expressed in CHO cells in at -80 mV holding potential by automated Qpatch clamp assay | | | |
| AID1852584 | Inhibition of hERG expressed in CHO cells Qpatch-clamp electrophysiology assay | | | |
| AID1892536 | Antiproliferative activity against human HUVEC cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID684471 | Displacement of [3H]GR113808 from human recombinant 5HT4c receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID684474 | Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP relative to 5HT | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID1275306 | Cmax in rat at 5 mg/kg, po | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1891110 | Inhibition of hERG channel expressed in HEK293 cells at -80 mV holding potential by automated patch clamp method | 2022 | European journal of medicinal chemistry, Jun-05, Volume: 236 | Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury. |
| AID1911590 | Inhibition of hERG channel assessed as prolongation of QT interval by patch clamp method | 2022 | Journal of medicinal chemistry, 06-09, Volume: 65, Issue:11
| Discovery of 1,6-Naphthyridin-2(1 |
| AID1275296 | Displacement of [3H]-GR113808 from human 5-HT4 receptor expressed in African green monkey COS7 cell membranes after 30 mins by liquid scintillation counting analysis | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID672177 | Inhibition of human ERG expressed in CHO cells at 3 uM | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID1506436 | Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting | | | |
| AID1886116 | Inhibition of human ERK potassium channel by automated patch clamp electrophysiology | | | |
| AID684475 | Inhibition of human ERG expressed in CHO cells at 3 uM | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID1892577 | Inhibition of human ERG potassium channel by manual patch-clamp electrophysiology | | | |
| AID684472 | Selectivity ratio of Ki for human 5HT3A receptor to Ki for human 5HT4c receptor | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID1683494 | Inhibition of human ERG | 2021 | Bioorganic & medicinal chemistry letters, 01-01, Volume: 31 | Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors. |
| AID1275299 | Induction of gastric emptying rate in Sprague-Dawley rat at 5 mg/kg, iv administered prior to feeding measured after 30 mins | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1275297 | Inhibition of human ERG channel by fluorescence polarization assay | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1884536 | Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by automated patch clamp method | 2022 | European journal of medicinal chemistry, Aug-05, Volume: 238 | Expansion of the S-CN-DABO scaffold to exploit the impact on inhibitory activities against the non-nucleoside HIV-1 reverse transcriptase. |
| AID684476 | Half life in rat liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID684473 | Agonist activity at human recombinant 5HT4c receptor expressed in HEK293 cells at 10-fold physiological level assessed as accumulation of cAMP | 2012 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
| Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation. |
| AID1892543 | Selectivity, ratio of IC50 for antiproliferative activity against human A2780 cells to IC50 for antiproliferative activity against human A2780/CDDP cells | | | |
| AID1878549 | Inhibition of human ERG | 2022 | Bioorganic & medicinal chemistry letters, 03-15, Volume: 60 | Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia. |
| AID1275304 | Half life in rat at 5 mg/kg, po | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID1892537 | Antiproliferative activity against human A2780 cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID1597588 | Inhibition of human ERG expressed in CHO cells at 0.1 uM incubated for 1 min at -80 mV holding potential by manual patch clamp assay relative to control | 2019 | European journal of medicinal chemistry, Sep-01, Volume: 177 | Development of the "hidden" multifunctional agents for Alzheimer's disease. |
| AID1892542 | Antiproliferative activity against human WI-38 cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID1880381 | Inhibition of human ERG potassium channel transfected in CHO cells by automated patch clamp assay | 2022 | Journal of medicinal chemistry, 06-23, Volume: 65, Issue:12
| Structure-Based Discovery of Novel NH |
| AID672178 | Half life in rat liver microsomes | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID672176 | Intrinsic activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation relative to 5HT | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID1506437 | Partial agonist activity at Rluc-tagged human 5-HT4 receptor expressed in human SH-5YSY cells co-expressing RGFP-fused to Gbeta1 assessed as inhibition of serotonin-induced coupling by BRET assay | | | |
| AID1814663 | Inhibition of hERG expressed in HEK293 cells | | | |
| AID1598932 | Inhibition of human ERG expressed in CHO cells at -80 mV holding potential measured after 3 mins by QPatch automated patch-clamp assay | 2019 | Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
| Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent. |
| AID672175 | Agonist activity at human 5HT4C receptor expressed at 100 fold physiological-level in HEK293 cells assessed as cAMP accumulation | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID1892545 | Antiproliferative activity against human T29 cells assessed as cell growth inhibition measured after 48 hrs by MTS assay | | | |
| AID1506435 | Agonist activity at human 5-HT4R expressed in GloSensor-22F6 expressing 2B2 cells co-expressing Galpha-s assessed as increase in cAMP accumulation up to 60 mins by luminometry relative to control 5-HT | | | |
| AID1275298 | Agonist activity at 5-HT4 receptor in rat esophageal thoracic muscularis mucosae assessed as carbachol-induced contraction | 2016 | European journal of medicinal chemistry, Feb-15, Volume: 109 | Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent. |
| AID672173 | Displacement of [3H]GR113808 from human recombinant 5HT4C receptor expressed in HEK293 cells | 2012 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
| Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749. |
| AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6
| A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |