| 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. |
| AID1196614 | Volume of distribution at steady state in male Wistar rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196598 | Inhibition of human ERG channel | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196623 | Oral bioavailability in male Wistar rat at 10 mg/kg | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196615 | Half life in male Wistar rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196606 | Genotoxicity in mouse L5178Ytk+/- cells assessed as occurrence of micronucleation event measured without metabolic activation at 28 ug/ml after 24 hrs by fluorescence/light microscopy with phase contrast | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196629 | Fraction unbound in human plasma at 1 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196609 | Anxiolytic activity in po dosed male Sprague-Dawley rat assessed as increase in drinking time after 1 hr by Vogel conflict test | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196599 | Intrinsic clearance in male rat liver microsomes at 1 uM during 30 mins incubation | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196600 | Intrinsic clearance in human liver microsomes at 1 uM during 30 mins incubation | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196620 | Cmax in male Wistar rat at 10 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196621 | Tmax in male Wistar rat at 10 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196595 | Displacement of [3H]MPEP from mGlu5 receptor (unknown origin) expressed in HEK293 cells by competition binding assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196597 | Displacement of [3H]flumazenil from rat cortex GABAA receptor BDZ binding site expressed in HEK293 cells by competition binding assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196627 | Fraction unbound in rat plasma at 1 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196622 | AUC (infinity) in male Wistar rat at 10 mg/kg, po | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196607 | Genotoxicity in mouse L5178Ytk+/- cells assessed as occurrence of micronucleation event measured with metabolic activation at 70 ug/ml after 24 hrs by fluorescence/light microscopy with phase contrast | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196626 | Fraction unbound in mouse plasma at 1 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196624 | Ratio of drug level in brain to plasma in male Wistar rat | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196625 | Ratio of drug level in CSF to plasma in male Wistar rat | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196596 | Negative allosteric modulation of mGlu5 (unknown origin) expressed in HEK293 cells assessed as inhibition of L-AP4-induced calcium mobilization incubated for 30 mins prior to L-AP4 induction by Fluo-4 AM staining-based fluorescence assay | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196608 | Metabolic stability in human liver microsomes assessed as level of GSH adduct at 20 uM at pH 7.4 after 60 mins by LC-MS/MS analysis relative to control | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196628 | Fraction unbound in cynomolgus monkey plasma at 1 uM by equilibrium dialysis method | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1196613 | Clearance in male Wistar rat at 2 mg/kg, iv | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2011 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 339, Issue:2
| CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. |
| AID1346269 | Human mGlu5 receptor (Metabotropic glutamate receptors) | 2015 | Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
| Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |
| AID1346275 | Mouse mGlu5 receptor (Metabotropic glutamate receptors) | 2011 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 339, Issue:2
| CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. |
| AID1346254 | Rat mGlu5 receptor (Metabotropic glutamate receptors) | 2011 | The Journal of pharmacology and experimental therapeutics, Nov, Volume: 339, Issue:2
| CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |