Results: 3

2.
Figure 3

Figure 3. From: Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.

A. Concentration-response curve of ML293 in human M4 cells in the presence of an EC20 concentration of ACh. B. ACh fold-shift assay for ML293 at a 30 µM concentration. Data represent three independent determinations performed in triplicate.

James M. Salovich, et al. Bioorg Med Chem Lett. ;22(15):5084-5088.
3.
Figure 2

Figure 2. From: Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.

Initial ACh EC20 triage screen of M4 analogs. Assay was performed at 10 µM using hM4-Gqi5-CHO cells; activity was monitored using an intracellular calcium mobilization assay. Values represent a single screening experiment performed in triplicate; numbered compounds were then reassessed using full concentration-response curves.

James M. Salovich, et al. Bioorg Med Chem Lett. ;22(15):5084-5088.

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