Assay ID | Title | Year | Journal | Article |
AID1183943 | Positive allosteric modulation of human mGlu2 receptor expressed in CHO cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184023 | Antagonist activity at 5HT2A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319678 | Positive allosteric modulation at human mGlu2 receptor F643A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184041 | Tmax in dog at 1 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183951 | AUC (0 to infinity) in Sprague-Dawley rat at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183991 | Selectivity for human mGlu2 receptor over ETA receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319683 | Lipophilicity, log P of the compound | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183994 | Selectivity for human mGlu2 receptor over H2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183993 | Selectivity for human mGlu2 receptor over H1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183946 | Metabolic stability in rat liver microsomes assessed as compound metabolized at 5 uM after 15 mins by MS/MS analysis in presence of NADPH | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183961 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on deep sleep stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184000 | Selectivity for human mGlu2 receptor over MC4 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184048 | Therapeutic index, ratio of cardiotoxicity in anesthetized guinea pig to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319688 | Fraction unbound in rat plasma assessed as free drug level at 5 uM by rapid equilibrium dialysis method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184047 | Therapeutic index, ratio of activity at rabbit purkinje fibre to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184027 | Plasma protein binding in human | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183975 | Selectivity for human mGlu2 receptor over 5HT1A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184029 | Plasma protein binding in mouse | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184031 | Apparent permeability from apical to basolateral side in human Caco2 cells | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184035 | Inhibition of human CYP3A4 (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319674 | Metabolic stability in rat liver microsomes assessed as compound metabolized at 5 uM measured after 15 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184042 | Elimination half life in dog at 1 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319684 | Dissociation constant, pKa of the compound | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183987 | Selectivity for human mGlu2 receptor over CCR1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319703 | Displacement of [3H]8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-phenyl-1-piperidinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine from mGlu2 receptor (unknown origin) | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183989 | Selectivity for human mGlu2 receptor over D2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319676 | Positive allosteric modulation of wild-type human mGlu2 receptor expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183969 | Binding affinity to rat mGlu6 receptor expressed in CHO cells assessed as calcium mobilization by [35S]GTPgamma binding assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184036 | Inhibition of human CYP2C9 (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184032 | Apparent permeability from basolateral to apical side in human Caco2 cells | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183948 | Clearance in Sprague-Dawley rat at 2.5 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319699 | Tmax in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319685 | Solubility of the compound in water at pH 7.4 | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184040 | Volume of distribution at steady state in dog at 1 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319689 | Fraction unbound in rat brain assessed as free drug level at 5 uM by rapid equilibrium dialysis method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319719 | Cmax in plasma of Sprague-Dawley rat sleep-wake EEG paradigm model as at 3 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183971 | Selectivity ratio of IC50 for human mGlu3 receptor to IC50 for human mGlu2 receptor | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319690 | Clearance in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184026 | Solubility of the compound in 20% HP-beta-CD at pH 4 | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184034 | Inhibition of human CYP2D6 (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183984 | Selectivity for human mGlu2 receptor over beta1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184010 | Selectivity for human mGlu2 receptor over V1A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184018 | Selectivity for human mGlu2 receptor over CICH receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184015 | Selectivity for human mGlu2 receptor over alpha2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183985 | Selectivity for human mGlu2 receptor over BK2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183944 | Positive allosteric modulation of human mGlu2 receptor expressed in CHO cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins relative to glutamate | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183962 | Dissociation constant, pKa of the compound | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319675 | Inhibition of human ERG expressed in HEK293 cells assessed as reduction in maximal tail current at 3 uM and holding potential of -60 mV measured after 5 mins by patch-clamp assay | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319697 | Clearance in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184051 | Genotoxicity in human TK6 cells up to 150 ug/ml by in vitro micronucleus test | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183958 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on passive wake stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183959 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on intermediate state at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183957 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on active wake stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319673 | Metabolic stability in human liver microsomes assessed as compound metabolized at 5 uM measured after 15 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184039 | Clearance in dog at 1 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183956 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as reduction in REM sleep at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319680 | Positive allosteric modulation at human mGlu2 receptor N735D mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183968 | Binding affinity to human mGlu4 receptor expressed in rat L929 cells assessed as calcium mobilization by [35S]GTPgamma binding assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184043 | AUC (0 to infinity) in dog at 2.5 mg/kg, po | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183999 | Selectivity for human mGlu2 receptor over M3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319691 | Elimination half life in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184016 | Selectivity for human mGlu2 receptor over BZD receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183979 | Selectivity for human mGlu2 receptor over 5HT7 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319677 | Positive allosteric modulation at human mGlu2 receptor L639A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183950 | Tmax in Sprague-Dawley rat at 2.5 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184038 | Volume of distribution at steady state in Sprague-Dawley rat at 2.5 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183986 | Selectivity for human mGlu2 receptor over CCKA receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183955 | Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat assessed effect on sleep-wake EEG paradigm after 20 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184003 | Selectivity for human mGlu2 receptor over NK3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183949 | Elimination half life in Sprague-Dawley rat at 2.5 mg/kg, iv | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319702 | Oral bioavailability in Beagle dog at 5 mg/kg | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183996 | Selectivity for human mGlu2 receptor over CXCR2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183982 | Selectivity for human mGlu2 receptor over A3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184019 | Selectivity for human mGlu2 receptor over GABA receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184045 | Oral bioavailability in dog at 2.5 mg/kg | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1607614 | Positive allosteric modulation of mGluR2 (unknown origin) relative to control | 2019 | Journal of medicinal chemistry, 07-11, Volume: 62, Issue:13
| Allosteric Modalities for Membrane-Bound Receptors: Insights from Drug Hunting for Brain Diseases. |
AID1184012 | Selectivity for human mGlu2 receptor over SST receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183967 | Binding affinity to human mGlu5 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319671 | Kinetic solubility of the compound in 20% HP-beta-cyclodextrin at pH 4 by UPLC/UV method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319701 | Cmax in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319682 | Positive allosteric modulation at human mGlu2 receptor F776A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183976 | Selectivity for human mGlu2 receptor over 5HT3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184001 | Selectivity for human mGlu2 receptor over NET (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184044 | Cmax in dog at 2.5 mg/kg, po | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319681 | Positive allosteric modulation at human mGlu2 receptor W773A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting metho | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319695 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183953 | Oral bioavailability in Sprague-Dawley rat at 10 mg/kg | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319700 | AUC (0 to infinity) in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184046 | Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat assessed free plasma drug level causing effect on sleep-wake EEG paradigm after 20 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184021 | Selectivity for human mGlu2 receptor over NaCH receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319698 | Half life in Beagle dog at 1 mg/kg, iv or 5 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319725 | Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat sleep-wake EEG paradigm model assessed as lowest active dose required to show effect on sleep-wake cycle by electroencephalogram analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183966 | Binding affinity to human mGlu3 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183995 | Selectivity for human mGlu2 receptor over IL8B receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183952 | Cmax in Sprague-Dawley rat at 10 mg/kg, po | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183965 | Binding affinity to human mGlu1 receptor expressed in HEK293 cells assessed as calcium mobilization by [35S]GTPgamma binding assay | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184037 | Inhibition of human CYP2C19 (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183960 | Positive allosteric modulation of mGlu2 receptor in Sprague-Dawley rat sleep-wake EEG paradigm model assessed as effect on light sleep stage at 3 mg/kg, po after 4 hrs by electroencephalogram analysis | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184024 | Selectivity for human mGlu2 receptor over 5HT2A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183980 | Selectivity for human mGlu2 receptor over A1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319692 | Tmax in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184022 | Selectivity for human mGlu2 receptor over SKCaCH receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184013 | Selectivity for human mGlu2 receptor over 5HT1B receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319694 | Cmax in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319669 | Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184052 | Genotoxicity in human TK6 cells up to 150 ug/ml by in vitro micronucleus test in presence of rat liver S9 fraction | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319679 | Positive allosteric modulation at wild type human mGlu2 receptor L732A mutant expressed in CHO-K1 cells assessed as potentiation of glutamate-induced effect preincubated for 30 mins prior to glutamate challenge measured after 30 mins by [35S]GTP-gammaS bi | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1183945 | Metabolic stability in human liver microsomes assessed as compound metabolized at 5 uM after 15 mins by MS/MS analysis in presence of NADPH | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184011 | Selectivity for human mGlu2 receptor over VIP receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183997 | Selectivity for human mGlu2 receptor over M1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183974 | Selectivity ratio of IC50 for rat mGlu6 receptor to IC50 for human mGlu2 receptor | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183977 | Selectivity for human mGlu2 receptor over 5HT5A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184008 | Selectivity for human mGlu2 receptor over OP3 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184006 | Selectivity for human mGlu2 receptor over NT1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184004 | Selectivity for human mGlu2 receptor over NPY1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184030 | Plasma protein binding in dog | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183990 | Selectivity for human mGlu2 receptor over DAT (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183988 | Selectivity for human mGlu2 receptor over D1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184020 | Selectivity for human mGlu2 receptor over KCH receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183964 | Displacement of [3H]19 from human mGlu2 receptor expressed in CHO cells | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184009 | Selectivity for human mGlu2 receptor over ORL1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183970 | Selectivity ratio of IC50 for human mGlu1 receptor to IC50 for human mGlu2 receptor | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184007 | Selectivity for human mGlu2 receptor over OP1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183983 | Selectivity for human mGlu2 receptor over AT1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184028 | Plasma protein binding in rat | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183981 | Selectivity for human mGlu2 receptor over A2A receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184025 | Solubility of the compound in water | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319696 | Ratio of drug level in brain to plasma of Swiss mouse at 10 mg/kg, sc measured after 1 hr | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184017 | Selectivity for human mGlu2 receptor over CaCH receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183973 | Selectivity ratio of IC50 for human mGlu4 receptor to IC50 for human mGlu2 receptor | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183954 | Ratio of drug level in brain to plasma in Swiss mouse at 10 mg/kg, sc after 1 hr | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319670 | Positive allosteric modulation of human mGlu2 receptor expressed in CHO cell membranes assessed as potentiation of glutamate-induced effect incubated for 30 mins prior to [35S]GTPgamma addition measured after 30 mins by scintillation counting method relat | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1319668 | Apparent permeability across apical to basolateral side over basolateral to apical side in human Caco2 cells at 1 uM measured after 120 mins | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184014 | Selectivity for human mGlu2 receptor over alpha1 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319726 | Positive allosteric modulation of mGlu2 receptor in po dosed Sprague-Dawley rat sleep-wake EEG paradigm model assessed as plasma concentration required to show effect on sleep-wake cycle by electroencephalogram analysis | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184002 | Selectivity for human mGlu2 receptor over NK2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183998 | Selectivity for human mGlu2 receptor over M2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319672 | Kinetic solubility of the compound at pH 7 by UPLC/UV method | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184049 | Therapeutic index, ratio of cardiotoxicity in anesthetized dog to efficacy free concentration in Sprague-Dawley rat sleep-wake EEG paradigm model | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183972 | Selectivity ratio of IC50 for human mGlu5 receptor to IC50 for human mGlu2 receptor | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319686 | Solubility of the compound in water at pH 2 | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184005 | Selectivity for human mGlu2 receptor over NPY2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183978 | Selectivity for human mGlu2 receptor over 5HT6 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183992 | Selectivity for human mGlu2 receptor over GAL2 receptor (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183963 | Lipophilicity, log P of the compound at pH 6.8 | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1184050 | Mutagenic activity in Salmonella typhimurium TA98 assessed as reverse mutation up to 125 ug/ml by Ames test | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1319693 | AUC (0 to infinity) in Sprague-Dawley rat at 2.5 mg/kg, iv or 10 mg/kg, po | 2016 | Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
| Discovery of 8-Trifluoromethyl-3-cyclopropylmethyl-7-[(4-(2,4-difluorophenyl)-1-piperazinyl)methyl]-1,2,4-triazolo[4,3-a]pyridine (JNJ-46356479), a Selective and Orally Bioavailable mGlu2 Receptor Positive Allosteric Modulator (PAM). |
AID1184033 | Inhibition of human CYP1A2 (unknown origin) | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
AID1183947 | Inhibition of human ERG channel transfected in HEK293 cells at 3 uM by patch clamp technique | 2014 | Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
| Discovery of 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone (JNJ-40411813): a novel positive allosteric modulator of the metabotropic glutamate 2 receptor. |
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. |
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. |
AID1346271 | Human mGlu2 receptor (Metabotropic glutamate receptors) | 2015 | Pharmacology research & perspectives, Feb, Volume: 3, Issue:1
| Pharmacological and pharmacokinetic properties of JNJ-40411813, a positive allosteric modulator of the mGlu2 receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |