Assay Detail
Binding
CHEMBL747492
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Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]OXO-M as the radioligand.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Muscarinic acetylcholine receptor M1 (CHEMBL276) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.90 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL115648 | — | — | 1 | 9.30 |
| CHEMBL331805 | — | — | 1 | 9.15 |
| CHEMBL21536 | XANOMELINE | 4.0 | 1 | 8.70 |
| CHEMBL332700 | — | — | 1 | 8.70 |
| CHEMBL2092949 | — | — | 1 | 8.60 |
| CHEMBL443282 | — | — | 1 | 8.40 |
| CHEMBL102560 | — | — | 1 | 8.40 |
| CHEMBL117666 | — | — | 1 | 8.35 |
| CHEMBL102588 | — | — | 1 | 8.34 |
| CHEMBL323719 | — | — | 1 | 8.30 |
| CHEMBL325964 | — | — | 1 | 8.25 |
| CHEMBL115473 | — | — | 1 | 8.22 |
| CHEMBL325225 | — | — | 1 | 8.05 |
| CHEMBL116462 | — | — | 1 | 8.00 |
| CHEMBL1788236 | — | — | 1 | 7.95 |
| CHEMBL117903 | — | — | 1 | 7.70 |
| CHEMBL105136 | — | — | 1 | 7.64 |
| CHEMBL115803 | — | — | 1 | 7.64 |
| CHEMBL117202 | — | — | 1 | 7.34 |
| CHEMBL327065 | — | — | 1 | 7.25 |
| CHEMBL117268 | — | — | 1 | 7.14 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 7.11 |
| CHEMBL115416 | — | — | 1 | 6.93 |
| CHEMBL117193 | — | — | 1 | 6.78 |
| CHEMBL117305 | — | — | 1 | 6.75 |
| CHEMBL74300 | — | — | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL115648 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL331805 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL21536 | XANOMELINE | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL332700 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2092949 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL443282 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL102560 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL117666 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL102588 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL323719 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL325964 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL115473 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL325225 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL116462 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1788236 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL117903 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL105136 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL115803 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL117202 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL327065 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL117268 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL115416 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL117193 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL117305 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL74300 | — | IC50 | = | 355.0 | nM | 6.45 |