Assay Detail
Binding
CHEMBL845360
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Binding affinity against muscarinic receptor in rat brain membranes using oxotremorine-M as ligand
41
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 8.01 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99240 | — | — | 1 | 9.14 |
| CHEMBL327269 | — | — | 1 | 9.10 |
| CHEMBL317324 | — | — | 1 | 8.92 |
| CHEMBL98255 | — | — | 1 | 8.92 |
| CHEMBL318403 | — | — | 1 | 8.89 |
| CHEMBL329924 | — | — | 1 | 8.89 |
| CHEMBL101054 | — | — | 1 | 8.85 |
| CHEMBL303922 | — | — | 1 | 8.80 |
| CHEMBL321073 | — | — | 1 | 8.77 |
| CHEMBL100147 | — | — | 1 | 8.77 |
| CHEMBL327754 | — | — | 1 | 8.70 |
| CHEMBL98529 | — | — | 1 | 8.37 |
| CHEMBL99521 | — | — | 1 | 8.33 |
| CHEMBL99476 | — | — | 1 | 8.24 |
| CHEMBL100253 | — | — | 1 | 8.23 |
| CHEMBL98843 | — | — | 2 | 8.22 |
| CHEMBL327289 | — | — | 1 | 8.21 |
| CHEMBL328828 | — | — | 1 | 8.10 |
| CHEMBL291351 | — | — | 1 | 8.07 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.01 |
| CHEMBL98750 | — | — | 1 | 7.89 |
| CHEMBL60419 | — | — | 1 | 7.85 |
| CHEMBL318718 | — | — | 1 | 7.85 |
| CHEMBL102088 | — | — | 1 | 7.82 |
| CHEMBL99768 | — | — | 1 | 7.70 |
| CHEMBL100163 | — | — | 1 | 7.70 |
| CHEMBL305401 | — | — | 1 | 7.66 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 7.64 |
| CHEMBL98759 | — | — | 1 | 7.64 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99240 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL327269 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL317324 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL98255 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL318403 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL329924 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL101054 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL303922 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL100147 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL321073 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL327754 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL98529 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL99521 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL99476 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL100253 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL98843 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL327289 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL328828 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL291351 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL98750 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL60419 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL318718 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL102088 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL98843 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL99768 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL100163 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL305401 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL14 | CARBACHOL | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL98759 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL330176 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL98757 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1169506 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL99884 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL99424 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL319109 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL550 | PILOCARPINE | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4524085 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL81878 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL316625 | — | IC50 | = | 363.0 | nM | 6.44 |