| Assay ID | Title | Year | Journal | Article |
|---|
| AID445675 | Antithromboembolism activity in EP3 gene knockout C57BL/6 mouse assessed as protection against arachidonic acid-induced mortality at 100 mg/kg, po administered 30 mins before arachidonic acid challenge | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID467787 | Displacement of [3H]PGE2 from human EP3 receptor | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists. |
| AID467788 | Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum | 2009 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
| Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists. |
| AID445684 | Inhibition of human CYP2C9 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445659 | Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445656 | Displacement of [3H]PGE2 from human EP3 receptor after 1 hr by liquid scintillation counting in presence of 10% human serum | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445674 | Antithromboembolism activity in EP3 gene knockout C57BL/6 mouse assessed as protection against arachidonic acid-induced mortality at 30 mg/kg, po administered 30 mins before arachidonic acid challenge | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445668 | Displacement of [3H]PGE2 from human EP3 receptor after 60 mins repeated washing by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445698 | Genotoxicity in Salmonella Typhimurium by Ames test | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445693 | Half life in dog at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445676 | Antiplatelet activity against human platelet rich plasma assessed as inhibition of collagen and sulprostone-induced platelet aggregation by platelet aggregometer | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445680 | Metabolic stability in monkey liver microsomes at 5 uM after 30 mins by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445666 | Selectivity ratio of IC50 for human EP3 receptor over IC50 for human IP receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445669 | Displacement of [3H]PGE2 from human EP1 receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445690 | Bioavailability in rat at 10 mg/kg | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445696 | Chronic toxicity in rat up to 150 mg/kg, po after 3 months | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445697 | Chronic toxicity in dog up to 20 mg/kg, po after 3 months | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445670 | Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445664 | Selectivity ratio of IC50 for human EP3 receptor over IC50 for human EP2 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445685 | Inhibition of human CYP2D6 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445678 | Metabolic stability in rat liver microsomes at 5 uM after 30 mins by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445681 | Metabolic stability in human liver microsomes at 5 uM after 30 mins by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445683 | Inhibition of human CYP2C19 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445686 | Inhibition of human CYP3A4 using dibenzylfluorescein as substrate | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445667 | Selectivity ratio of IC50 for human EP3 receptor over IC50 for mouse FP3 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445663 | Selectivity ratio of IC50 for human EP3 receptor over IC50 for human EP1 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445688 | Permeability across human Caco-2 cell membrane | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445677 | Metabolic stability in mouse liver microsomes at 5 uM after 30 mins by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445695 | Cmax in dog at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445665 | Selectivity ratio of IC50 for human EP3 receptor over IC50 for human EP4 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID474886 | Inhibition of PGE2-induced uterine contraction in pregnant rat at 3 mg/kg, po after 4 hrs | 2010 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 20, Issue:8
| Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists. |
| AID445691 | Bioavailability in dog at 10 mg/kg | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445694 | Cmax in rat at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445692 | Half life in rat at 10 mg/kg, po | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445682 | Inhibition of human CYP1A2 | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445689 | Solubility in water at pH 7 by shake flask method | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445687 | Inhibition of human CYP3A4 using 7-benzyloxy-4-trifluoromethylcoumarin as substrate | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445671 | Displacement of [3H]PGE2 from human EP4 receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445679 | Metabolic stability in dog liver microsomes at 5 uM after 30 mins by LC-MS/MS analysis | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445672 | Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445673 | Displacement of [3H]PGE2 from mouse EP3 receptor after 1 hr by liquid scintillation counting | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID445655 | Ratio of IC50 for human EP3 receptor in presence of 10% human serum to IC50 for human EP3 receptor | 2010 | Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
| Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor an |
| AID1346343 | Human EP3 receptor (Prostanoid receptors) | 2008 | American journal of physiology. Renal physiology, Oct, Volume: 295, Issue:4
| Modulation of bladder function by prostaglandin EP3 receptors in the central nervous system. |
| AID1346343 | Human EP3 receptor (Prostanoid receptors) | 2009 | British journal of pharmacology, Sep, Volume: 158, Issue:1
| Dual modulation of urinary bladder activity and urine flow by prostanoid EP3 receptors in the conscious rat. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |