| Assay ID | Title | Year | Journal | Article |
|---|
| AID371759 | Tmax in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371747 | Selectivity ratio of EC50 for rat muscarinic M2 receptor to EC50 for human muscarinic M5 receptor | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371757 | Cmax in Sprague-Dawley rat plasma at 10 mg/kg, ip within 1 hr | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746441 | Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID371751 | Intrinsic activity at human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein up to 30 uM by calcium mobilization assay in absence of acetylcholine | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746449 | Positive allosteric modulation of human muscarinic M1 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID371734 | Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371742 | Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371761 | Elimination half life in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID453991 | Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization at 30 uM | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID371743 | Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization at 30 uM relative to acetylcholine | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746445 | Positive allosteric modulation of rat muscarinic M5 receptor relative to acetylcholine | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID675658 | Positive allosteric modulation activity at muscarinic M5 receptor | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. |
| AID372002 | Apparent oral volume of distribution in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746446 | Positive allosteric modulation of human muscarinic M3 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID746451 | Positive allosteric modulation of human muscarinic M5 receptor assessed as fold shift of acetylcholine-induced response at 30 uM | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID675659 | Positive allosteric modulation activity at muscarinic M5 receptor relative to acetylcholine | 2012 | Journal of medicinal chemistry, Feb-23, Volume: 55, Issue:4
| Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery. |
| AID371749 | Selectivity ratio of EC50 for rat muscarinic M4 receptor to EC50 for human muscarinic M5 receptor | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID453994 | Ratio of AUC in rat brain to AUC in rat plasma | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID371738 | Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371735 | Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization at 30 uM relative to acetylcholine | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371755 | Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein by scintillation counting in presence of acetylcholine | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746443 | Positive allosteric modulation of rat muscarinic M5 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID374755 | Ratio of AUC (0 to 6 hrs) in Sprague-Dawley rat brain to AUC (0 to 6 hrs) in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID453989 | Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID371760 | Tmax in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746452 | Positive allosteric modulation of human muscarinic M5 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID453992 | Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization at 30 uM | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID371750 | Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine potency at 30 uM by calcium mobilization-based ACh concentration-response curve assay relative to control | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371748 | Selectivity ratio of EC50 for human muscarinic M3 receptor to EC50 for human muscarinic M5 receptor | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371745 | Activation of rat muscarinic M4 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization up to 30 uM | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371765 | Apparent oral clearance in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371753 | Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein up to 30 uM by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID453987 | Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID371744 | Activation of rat muscarinic M2 receptor expressed in CHO cells coexpressing chimeric Gqi5 protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization up to 30 uM | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371758 | Cmax in Sprague-Dawley rat brain at 10 mg/kg, ip within 1 hr | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371764 | AUC (0 to 6 hrs) in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371756 | Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine affinity at 30 uM by [3H]NMS competition binding assay relative to control | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746450 | Positive allosteric modulation of human muscarinic M5 receptor relative to acetylcholine | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID746448 | Positive allosteric modulation of human muscarinic M2 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID371752 | Displacement of [3H]NMS from human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein by scintillation counting | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371763 | AUC (0 to 6 hrs) in Sprague-Dawley rat plasma at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID371762 | Elimination half life in Sprague-Dawley rat brain at 10 mg/kg, ip | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID746447 | Positive allosteric modulation of human muscarinic M4 receptor | 2013 | Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10
| Discovery of ML326: The first sub-micromolar, selective M5 PAM. |
| AID371746 | Selectivity ratio of EC50 for rat muscarinic M1 receptor to EC50 for human muscarinic M5 receptor | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| AID453990 | Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization | 2010 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
| Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. |
| AID1345543 | Human M5 receptor (Acetylcholine receptors (muscarinic)) | 2009 | Journal of medicinal chemistry, Jun-11, Volume: 52, Issue:11
| Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |