AID132457 | The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intracerebroventricular), for 5 min drug pretreatment time | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID1137663 | Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by competition binding assay | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17. |
AID143765 | Selectivity ratio for CPP and gly NMDA binding | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| 3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex. |
AID1385406 | Agonist activity at mouse GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID71953 | Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in porcine kidney | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
AID234200 | Ratio of the inhibitory activity against [3H]-CCP for rat cortical and hippocampal membrane glutamate binding site to [3H]glycine for rat cortical and hippocampal membrane binding site. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID1385417 | Selectivity ratio of EC50 for mouse GPR17 expressed in HEK293 cells to EC50 for human GPR17 expressed in human 1321N1 cells | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID71952 | Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in human liver | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
AID132459 | The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intravenous), for 5 min drug pretreatment time | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID1385405 | Agonist activity at rat GPR17 expressed in HEK293 cells assessed as induction of intracellular calcium mobilization by calcium 5-dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID145260 | In vitro inhibition of [3H]glycine at NMDA receptor | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. |
AID684832 | Inhibition of human recombinant FBPase using fructose-1,6-biphosphate as substrate incubated for 3 mins prior to substrate addition by spectrophotometric analysis | 2012 | European journal of medicinal chemistry, Oct, Volume: 56 | Ligand-based designing, in silico screening, and biological evaluation of new potent fructose-1,6-bisphosphatase (FBPase) inhibitors. |
AID1385416 | Selectivity ratio of EC50 for rat GPR17 expressed in HEK293 cells to EC50 for human GPR17 expressed in human 1321N1 cells | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID1385403 | Displacement of [3H]CCP from NMDA receptor glutamate binding site in rat cortical and hippocampal membranes | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID1385413 | Agonist activity at human P2Y12 receptor transfected in CHO cells assessed as induction of beta-arrestin translocation | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID1137662 | Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes assessed as dissociation half life at 100 uM treated after 1 hr incubation with radioligand by liquid scintillation counting | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17. |
AID1385411 | Agonist activity at human P2Y4 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UTP by fluo-4 dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID1137661 | Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes assessed as association half life at 100 uM by liquid scintillation counting | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17. |
AID227647 | Activity was determined by inhibition of glutamate stimulated accumulation of cyclic GMP in neonatal rat cerebral slices. | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| 3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex. |
AID1385402 | Displacement of [3H]glycine from NMDA receptor in rat cortical and hippocampal membranes | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID132458 | The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid seizure model (intraperitoneal), for 2 hr drug pretreatment time | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID131549 | Protection from audiogenic seizure in the DBA/2 mouse 30 min after intraperitoneal administration | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
| 3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor. |
AID92506 | The compound was evaluated in vivo for the competitive binding against [3H]-Ionotropic glutamate receptor AMPA for rat cortical and hippocampal membrane glutamate binding site. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID1385409 | Agonist activity at human P2Y1 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of ADP by fluo-4 dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID186995 | Blockade of NMDA-induced depolarizations on rat cortical slices | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
| 3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor. |
AID143231 | Compound was evaluated for in vitro inhibition of cGMP cerebellar slice at NMDA receptor. | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. |
AID1137664 | Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by homologous competition binding assay in presence of pranlukast | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4
| Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17. |
AID71955 | Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in rabbit liver | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
AID1076089 | Inhibition of human recombinant FBPase expressed in Escherichia coli BL21(DE3) by phosphoglucose isomerase and glucose-6-phosphate dehydrogenase coupled assay | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
| Design, synthesis and biological evaluation of 7-nitro-1H-indole-2-carboxylic acid derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase. |
AID1189736 | Inhibition of human liver FBPase expressed in Escherichia coli BL21(DE3) Rosetta cells assessed as reduction of NADP+ to NADPH by phosphoglucose isomerase and glucose-6-phosphate dehydrogenase coupling based spectrophotometry | 2015 | European journal of medicinal chemistry, Jan-27, Volume: 90 | Discovery of novel indole derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase. |
AID1385412 | Agonist activity at human P2Y6 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UDP by fluo-4 dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID143618 | Ability to compete with [3H]glycine for strychnine-insensitive binding sites on rat cortical and hippocampal membrane | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID112660 | In vivo antagonist activity against seizures elicited by audiogenic administered icv in mice | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. |
AID143610 | Inhibition of binding of [3H]glycine to N-methyl-D-aspartate glutamate receptor 1 from crude synaptic membranes prepared from adult rat cerebral cortex. | 1998 | Journal of medicinal chemistry, Mar-12, Volume: 41, Issue:6
| (E)-3-(2-(N-phenylcarbamoyl)vinyl)pyrrole-2-carboxylic acid derivatives. A novel class of glycine site antagonists. |
AID1385414 | Agonist activity at human P2Y14 receptor transfected in CHO cells assessed as induction of beta-arrestin translocation | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID1385418 | Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO cell membranes after 60 mins by liquid scintillation counting | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID143068 | Inhibition of the binding of [3H]L-689,560 ([3H]-4) to the strychnine-insensitive glycine site on rat brain membranes | 1994 | Journal of medicinal chemistry, May-13, Volume: 37, Issue:10
| 3'-(Arylmethyl)- and 3'-(aryloxy)-3-phenyl-4-hydroxyquinolin-2(1H)-ones: orally active antagonists of the glycine site on the NMDA receptor. |
AID1385410 | Agonist activity at human P2Y2 receptor transfected in human 1321N1 cells assessed as induction of calcium mobilization after 30 mins in presence of UTP by fluo-4 dye based assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
| 3-(2-Carboxyethyl)indole-2-carboxylic Acid Derivatives: Structural Requirements and Properties of Potent Agonists of the Orphan G Protein-Coupled Receptor GPR17. |
AID132456 | The compound was evaluated in vivo for the anticonvulsant activity in quinolinic acid + probenecid seizure model (intravenous), for 5 min drug pretreatment time | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID132454 | The compound was evaluated in vivo for the anticonvulsant activity in audiogenic seizure model (intraperitoneal), for 2 hr drug pretreatment time | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID71956 | Inhibitory activity against Fructose-1,6-bisphosphatase (F16BPase) in rat liver | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
AID143472 | Activity against rat cortical and hippocampal membrane strychnine-insensitive N-methyl-D-aspartate glutamate receptor 1 using [3H]-gly | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| 3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex. |
AID143781 | Activity against rat cortical and hippocampal membrane N-methyl-D-aspartate glutamate receptor 1/2A/2B/2C/2D using [3H]CPP | 1990 | Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
| 3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex. |
AID112661 | In vivo antagonist activity against seizures elicited by audiogenic administered intra peritoneally in mice | 1994 | Journal of medicinal chemistry, Nov-25, Volume: 37, Issue:24
| The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. |
AID143790 | Ability to compete with [3H]CCP for rat cortical and hippocampal membrane glutamate binding site. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID93726 | The compound was evaluated in vivo for the competitive binding against [3H]kainate for rat cortical and hippocampal membrane glutamate binding site. | 1992 | Journal of medicinal chemistry, May-15, Volume: 35, Issue:10
| 3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site. |
AID1076090 | Inhibition of FBPase (unknown origin) | 2014 | Bioorganic & medicinal chemistry, Mar-15, Volume: 22, Issue:6
| Design, synthesis and biological evaluation of 7-nitro-1H-indole-2-carboxylic acid derivatives as allosteric inhibitors of fructose-1,6-bisphosphatase. |
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. |
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. |
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. |
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. |
AID977608 | Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB | 2003 | Bioorganic & medicinal chemistry letters, Jun-16, Volume: 13, Issue:12
| 3-(2-carboxyethyl)-4,6-dichloro-1H-indole-2-carboxylic acid: an allosteric inhibitor of fructose-1,6-bisphosphatase at the AMP site. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |