| 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. |
| AID618715 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced calcium mobilization after 1 hr by FLIPR assay | 2011 | Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
| Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. |
| AID420564 | Ratio of AUC (0 to 8 hrs) in Sprague-Dawley rat brain to AUC (0 to 8 hrs) in Sprague-Dawley rat plasma | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420553 | Fraction unbound in human plasma by at 10 mM | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID618716 | Positive allosteric modulation of human mGlu4 receptor expressed in BHK cells assessed as potentiation of glutamate-induced response after 1 hr by FLIPR assay relative to glutamate | 2011 | Journal of medicinal chemistry, Jul-28, Volume: 54, Issue:14
| Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. |
| AID420537 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420539 | Activity at human mGluR8 assessed as fold shifting of glutamate-induced response to left | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID1169627 | Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID632375 | Inhibition of CYP3A4 in human liver microsomes using 1-hydroxymidazolam as substrate | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 ( |
| AID420561 | Half life in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420546 | Activity at rat mGluR4 expressed in HEK293 cells coexpressing Gqi5 protein assessed as fold shifting of glutamate-induced response to left at 30 uM | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420559 | AUC in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420541 | Activity at human mGluR5 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID1242927 | Displacement of [3H]N-(4-chloro-3-methoxyphenyl)picolinamide from human mGlu4 receptor expressed in CHO cell membranes incubated for 30 mins by liquid scintillation counting method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
| Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID631414 | Inhibition of CYP2D6 in human liver microsomes using dextrophan tartarate as substrate | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 ( |
| AID420549 | Selectivity ratio of human mGluR4 to human mGluR5 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID1242928 | Half life in Wistar rat liver microsomes in presence of NADPH generation system by HPLC method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
| Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID420560 | AUC in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420562 | Half life in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420542 | Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID771114 | Antagonist activity at mGlu8 receptor (unknown origin) expressed in CHO cells assessed as inhibition of glutamate-induced inositol phosphate accumulation at 10 uM after 45 mins by liquid scintillation counting analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Radiosynthesis of N-(4-chloro-3-[(11)C]methoxyphenyl)-2-picolinamide ([(11)C]ML128) as a PET radiotracer for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID420550 | Selectivity ratio of human mGluR4 to human mGluR8 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420545 | Activity at human mGluR4 expressed in CHO cells coexpressing Gqi5 protein assessed as fold shifting of glutamate-induced response to left at 30 uM | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420558 | Tmax in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID631413 | Inhibition of CYP2C9 in human liver microsomes using 4-hydroxydiclofenac as substrate | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 ( |
| AID420547 | Activity at human mGluR1 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420543 | Activity at human mGluR4 receptor expressed in CHO cells assessed as effect on calcium mobilization relative to glutamate | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID771117 | Agonist activity at mGlu5a receptor (unknown origin) expressed in CHO cells assessed as induction of inositol phosphate accumulation at 10 uM after 45 mins by liquid scintillation counting analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Radiosynthesis of N-(4-chloro-3-[(11)C]methoxyphenyl)-2-picolinamide ([(11)C]ML128) as a PET radiotracer for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID1169628 | Displacement of [3H]ML128 from rat mGlu4 receptor expressed in CHO cells at 10 uM after 30 mins by liquid scintillation counting analysis | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
| Radiosynthesis and evaluation of an 18F-labeled positron emission tomography (PET) radioligand for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID420548 | Activity at human mGluR2 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID771115 | Antagonist activity at mGlu5a receptor (unknown origin) expressed in CHO cells assessed as inhibition of glutamate-induced inositol phosphate accumulation at 10 uM after 45 mins by liquid scintillation counting analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Radiosynthesis of N-(4-chloro-3-[(11)C]methoxyphenyl)-2-picolinamide ([(11)C]ML128) as a PET radiotracer for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID1242929 | Effective permeability by PAMPA method | 2015 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
| Re-exploring the N-phenylpicolinamide derivatives to develop mGlu4 ligands with improved affinity and in vitro microsomal stability. |
| AID420538 | Activity at human mGluR7 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420540 | Activity at human mGluR3 | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420557 | Tmax in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420563 | Apparent oral clearance in Sprague-Dawley rat at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420552 | Metabolic stability in rat liver microsomes after 1 hr | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420554 | Fraction unbound in rat plasma by at 10 mM | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID771116 | Agonist activity at mGlu8 receptor (unknown origin) expressed in CHO cells assessed as induction of inositol phosphate accumulation at 10 uM after 45 mins by liquid scintillation counting analysis relative to control | 2013 | Bioorganic & medicinal chemistry, Oct-01, Volume: 21, Issue:19
| Radiosynthesis of N-(4-chloro-3-[(11)C]methoxyphenyl)-2-picolinamide ([(11)C]ML128) as a PET radiotracer for metabotropic glutamate receptor subtype 4 (mGlu4). |
| AID420556 | Cmax in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420544 | Activity at rat mGluR4 receptor expressed in HEK293 cells assessed as effect on thallium flux relative to glutamate | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID420555 | Cmax in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID631412 | Inhibition of CYP1A2 in human liver microsomes using acetaminophen as substrate | 2011 | Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
| Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 ( |
| AID420551 | Metabolic stability in human liver microsomes after 1 hr | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| AID1346285 | Human mGlu4 receptor (Metabotropic glutamate receptors) | 2009 | Journal of medicinal chemistry, Jul-23, Volume: 52, Issue:14
| Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |