Assay ID | Title | Year | Journal | Article |
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. |
AID1171997 | Positive allosteric modulator activity at human muscarinic receptor subtype 1 expressed in CHO-K1 cells by calcium mobilization assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
| Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators. |
AID463620 | Potentiation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization up to 30 uM after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
AID721557 | Positive allosteric modulator activity at human muscarinic M1 receptor by calcium mobilization assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. |
AID675655 | Positive allosteric modulation activity at muscarinic M1 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. |
AID731234 | Positive allosteric modulation of human muscarinic M1 receptor assessed as leftward fold shift of acetylcholine-induced response at 30 uM relative to acetylcholine | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. |
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. |
AID721555 | Positive allosteric modulator activity at human muscarinic M1 receptor relative to acetylcholine by calcium mobilization assay | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. |
AID463612 | Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay relative to acetylcholine | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 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. |
AID463618 | Potentiation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization up to 30 uM after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
AID463614 | Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization at 30 uM after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
AID463619 | Potentiation of muscarinic M4 receptor expressed in CHO cells co-transfected with Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization up to 30 uM after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
AID675654 | Positive allosteric modulation activity at muscarinic M1 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. |
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. |
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. |
AID463611 | Potentiation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
AID731231 | Positive allosteric modulation of human muscarinic M1 receptor | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. |
AID731232 | Positive allosteric modulation of human muscarinic M1 receptor relative to acetylcholine | 2013 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 23, Issue:6
| Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule. |
AID463617 | Potentiation of muscarinic M2 receptor expressed in CHO cells co-transfected with Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization up to 30 uM after 1 hr by FLIPR assay | 2010 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
| Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. |
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. |
AID595144 | Ratio of AUC in brain to plasma in rat at 10 mg/kg, ip after 1 hr | 2011 | Bioorganic & medicinal chemistry letters, May-01, Volume: 21, Issue:9
| Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. |
AID721554 | Positive allosteric modulator activity at human muscarinic M1 receptor assessed as fold shift of acetylcholine concentration curve to the left at 30 uM by calcium mobilization assay relative to untreated acetylcholine control | 2013 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 23, Issue:2
| Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |