| 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. |
| 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. |
| 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. |
| AID611784 | Agonist activity at rat GluK2 mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID611792 | Agonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281135 | Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx at 100 uM by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID611788 | Displacement of [3H]SYM2081 from rat GluK3 expressed in Sf9 cells | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID611795 | Agonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes at 1 mM by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281125 | Antagonist activity at mGlu1 receptor assessed as inhibition of DHPG-induced depolarization of neonatal rat motoneurons at 10 uM | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281120 | Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281133 | Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281122 | Antagonist activity at native AMPA receptor assessed as fDR-VRP reduction of neonatal rat spinal cord motorneurones | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281131 | Antagonist activity at human recombinant GLUK5/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281127 | Antagonist activity at mGlu5 receptor assessed as inhibition of DHPG-induced depolarization of neonatal rat spinal cord motoneurons at 10 uM | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID611794 | Antagonist activity at non-desensitized homomeric rat GluK3 mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281129 | Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID611789 | Ratio of Ki for rat GluA2 to Ki for rat GluK1 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281123 | Antagonist activity at NMDA receptor assessed as inhibition of NMDA-induced depolarization of neonatal rat spinal cord motoneurons at 10 uM | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID611796 | Antagonist activity at Non-desensitized homomeric rat GluK1(Q)1b mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID611790 | Ratio of Ki for rat GluK3 to Ki for rat GluK2 | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281121 | Activity at native AMPA receptor assessed as antagonism of (S)-5-fluoriwillardiine-induced depolarization of neonatal rat spinal cord motorneurones | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID611793 | Antagonist activity at non-desensitized homomeric rat GluK2 mutant expressed in Xenopus oocytes assessed as inhibition of (S)-glutamate-induced current by two-electrode voltage-clamp electrophysiology | 2011 | Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
| Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization. |
| AID281134 | Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID281130 | Antagonist activity at human recombinant GLUK5 receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay | 2007 | Journal of medicinal chemistry, Apr-05, Volume: 50, Issue:7
| Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists. |
| AID1346569 | Human GluK1 (Ionotropic glutamate receptors) | 2010 | Molecular pharmacology, Dec, Volume: 78, Issue:6
| Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310. |
| AID1346566 | Human GluK3 (Ionotropic glutamate receptors) | 2010 | Molecular pharmacology, Dec, Volume: 78, Issue:6
| Mapping the ligand binding sites of kainate receptors: molecular determinants of subunit-selective binding of the antagonist [3H]UBP310. |
| AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2006 | The Journal of neuroscience : the official journal of the Society for Neuroscience, Mar-15, Volume: 26, Issue:11
| Crystal structures of the kainate receptor GluR5 ligand binding core dimer with novel GluR5-selective antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |