| Assay ID | Title | Year | Journal | Article |
|---|
| AID594734 | Binding affinity to 5-HT6 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594736 | Agonist activity at human muscarinic M4 receptor up to 10 uM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594731 | Binding affinity to muscarinic M4 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594741 | Increase of peak urethral pressure in iv dosed anesthetized dog stress urinary incontinence model at 20 to 45 nM of free plasma concentration relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594668 | Plasma protein binding in rat | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594669 | Plasma protein binding in dog | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594583 | Agonist activity at human 5HT2B receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization at 10 uM by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594751 | Inhibition of 5HT2A receptor-mediated head twitches in rat at 10 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594740 | Inhibition of Nav1.5 in rabbit cardiac myocytes up to 100 uM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594739 | Inhibition of human ERG by patch-clamp method | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594593 | Agonist activity at human recombinant 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594750 | Agonist activity at 5HT2A receptor in dog femoral artery | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594728 | Oral bioavailability in CD rat at 2 mg/kg administered as single dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594648 | Inhibition of CYP2C9 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594581 | Displacement of [3H]meselurgine from human 5HT2C receptor expressed in Swiss mouse 3T3 cells by scintillation proximity assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594595 | Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154576 | Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594666 | Intrinsic clearance in rat hepatocytes assessed per 10'6 cells | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594664 | Intrinsic clearance in rat liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594753 | Cardiotoxicity in anaesthetized dog assessed as effect on blood pressure up to 0.5 mg/kg, iv administered as infusion over 60 mins | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594656 | Binding affinity to sodium channel site 2 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594748 | Dissociation constant, pKa of the compound | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594671 | Elimination half life in Beagle dog at 0.030 mg/kg, iv administered as single infusion over 1 hr | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594580 | Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594724 | Volume of distribution in Beagle dog at 0.030 mg/kg, iv administered as infusion over 1 hr | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154582 | Agonist activity at 5-HT2A receptor in beagle dog femoral arteries tissue after 1 hr | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID1154577 | Agonist activity at recombinant human 5-HT2C receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay relative to 5HT | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594590 | Lipophilicity, log D of the compound at pH 7.4 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594670 | Elimination half life in CD rat at 1 mg/kg, iv administered as single bolus dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594644 | Agonist activity at human recombinant 5HT2B receptor expressed in Swiss mouse 3T3 cells assessed as increase of fluorescence based calcium mobilization at 10 uM by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594733 | Binding affinity to 5-HT3 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594646 | Intrinsic clearance in human hepatocytes assessed per 10'6 cells | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594672 | Plasma clearance in CD rat at 1 mg/kg, iv administered as single bolus dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594650 | Inhibition of CYP2D6 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594594 | Agonist activity at human recombinant 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594647 | Inhibition of CYP1A2 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154578 | Octanol-water partition coefficient, log D of the compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594653 | Apparent permeability from apical to basolateral side in MDCK2 cells expressing MDR1 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594730 | Binding affinity to muscarinic M3 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594663 | Binding affinity to L-type Ca2+ channel dihydropyridine binding site at 10000 nM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594657 | Binding affinity to L-type calcium channel diltiazem binding site | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594674 | Volume of distribution in CD rat at 1 mg/kg, iv administered as single bolus dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594651 | Inhibition of CYP3A4 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594662 | Binding affinity to L-type calcium channel verapamil binding site at 10000 nM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594754 | Cardiotoxicity in anaesthetized dog assessed as effect on heart rate up to 0.5 mg/kg, iv administered as infusion over 60 mins | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594737 | Agonist activity at human muscarinic M5 receptor up to 10 uM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594743 | Agonist activity at dog 5HT2C receptor ralative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154585 | Ratio of fraction unbound in iv dosed beagle dog CSF to fraction unbound in iv dosed beagle dog plasma | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594727 | AUC (0 to infinity) in CD rat at 2 mg/kg, po administered as single dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594591 | Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154580 | Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594726 | Tmax in CD rat at 2 mg/kg, po administered as single dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154581 | Agonist activity at recombinant human 5-HT2B receptor expressed in CHO K1 cells assessed as calcium mobilization by FLIPR assay relative to 5HT | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594725 | Cmax in CD rat at 2 mg/kg, po administered as single dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594749 | Drug excretion in CD rat urine at 1 mg/kg, iv administered as single bolus dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594732 | Binding affinity to muscarinic M5 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1627015 | Intrinsic clearance in human liver microsomes | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
| AID594645 | Intrinsic clearance in human liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594729 | Binding affinity to muscarinic M1 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1627017 | Permeability in RRCK cells | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
| AID594742 | Agonist activity at dog 5HT2C receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594673 | Plasma clearance in Beagle dog at 0.030 mg/kg, iv administered as infusion over 1 hr | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594661 | Binding affinity to L-type calcium channel diltiazem binding site at 10000 nM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154583 | Agonist activity at 5-HT2A receptor in beagle dog femoral arteries tissue after 1 hr relative to 5HT | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594578 | Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594752 | Agonist activity at 5HT2A receptor in dog femoral artery relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594814 | Increase of peak urethral pressure in iv dosed anesthetized dog stress urinary incontinence model | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594654 | Apparent permeability basolateral to apical side in MDCK cells expressing MDR1 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1154584 | Efflux ratio of permeability from basolateral to apical side to apical to basolateral side in MDCK cells expressing MDR1 | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
| Multiparameter optimization in CNS drug discovery: design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT₂C) receptor agonists with exquisite functional selectivity over 5-HT₂A and 5-HT₂B receptors. |
| AID594735 | Agonist activity at human muscarinic M1 receptor up to 10 uM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594652 | Apparent permeability of the compound by PAMPA | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594665 | Intrinsic clearance in dog liver microsomes | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594659 | Binding affinity to L-type calcium channel dihydropyridine binding site | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594592 | Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594813 | Ratio of free drug level in brain to plasma in CD rat at 10 mg/kg, po administered as single dose | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594649 | Inhibition of CYP2C19 | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594596 | Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay relative to control | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID1627012 | Displacement of [3H]-mesulergine from recombinant human 5-HT2C receptor transfected in Swiss mouse 3T3 cells after 150 mins by scintillation proximity assay | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
| Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines. |
| AID594658 | Binding affinity to L-type calcium channel verapamil binding site | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594667 | Intrinsic clearance in dog hepatocytes assessed per 10'6 cells | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594738 | Antagonist activity at human muscarinic M4 receptor | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594655 | Binding affinity to human ERG | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| AID594660 | Binding affinity to sodium channel site 2 at 10000 nM | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
| 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. |
| 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |