[3H]PT-1284 displacement binding to hM1 mAChR membranes by positive allosteric modulators and orthosteric or allosteric binding ligands
[3H]PT-1284 displacement binding values (pKi) were obtained in the presence of 1 mM ACh. Data shown are the result of three separate experiments performed in duplicate and expressed as the mean pKi ± S.D.
| Compound ID | Binding Site | pKi | Reference |
|---|---|---|---|
| PT-1284 (1) | PAM | 5.97 ± 0.19 | WO2012003147 |
| Compound 2 | PAM | 8.15 ± 0.23 | WO2011084368 |
| Compound 3 | PAM | 8.09 ± 0.02 | WO2011084368 |
| Compound 4 | PAM | 7.99 ± 0.27 | WO2012003147 |
| Compound 5 | PAM | 7.51 ± 0.07 | WO2014077401 |
| Compound 6 | PAM | 7.45 ± 0.08 | WO2011084368 |
| Compound 7 | PAM | 7.28 ± 0.19 | WO2011084368 |
| PF-06764427 | PAM | 6.92 ± 0.23 | Sigma #PZ0300 |
| Compound 8 | PAM | 6.61 ± 0.21 | WO2013091773 |
| AZD6088 | Allosteric Agonist | 5.53 ± 0.19 | WO2009034380 |
| Danipon | Allosteric Agonist | <5.00 | (Sumiyoshi et al., 2013) |
| GSK1034702 | Allosteric Agonist | <5.00 | (Budzik et al., 2010) |
| TBPB | Allosteric Agonist | 5.57 ± 0.05 | Sigma no. SML0453 |
| Xanomeline | Orthosteric Agonist | 5.58 ± 0.15 | Sigma no. X2754 |
| Oxotremorine | Orthosteric Agonist | <5.00 | Tocris no. 0843 |
| Carbachol | Orthosteric Agonist | <5.00 | Sigma no. C4382 |