Assay Detail
Binding
CHEMBL748599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for muscarinic receptor in rat brain was measured by inhibition of [3H](R)-quinuclidinyl benzilate (QNB) binding
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Muscarinic acetylcholine receptor (CHEMBL1907609) ↗| Type | PROTEIN FAMILY |
| Organism | Rattus norvegicus |
Publication
Design, synthesis, and neurochemical evaluation of 2-amino-5-(alkoxycarbonyl)-3,4,5,6-tetrahydropyridines and 2-amino-5-(alkoxycarbonyl)-1,4,5,6-tetrahydropyrimidines as M1 muscarinic receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.28 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.00 |
| CHEMBL540315 | — | — | 1 | 5.77 |
| CHEMBL541398 | — | — | 1 | 5.66 |
| CHEMBL557795 | — | — | 1 | 5.64 |
| CHEMBL544556 | — | — | 1 | 5.62 |
| CHEMBL537928 | — | — | 1 | 5.48 |
| CHEMBL542065 | — | — | 1 | 5.48 |
| CHEMBL540567 | — | — | 1 | 5.37 |
| CHEMBL545725 | — | — | 1 | 5.32 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.26 |
| CHEMBL543614 | — | — | 1 | 5.09 |
| CHEMBL538467 | — | — | 1 | 5.04 |
| CHEMBL553602 | — | — | 1 | 5.00 |
| CHEMBL538224 | — | — | 1 | 4.66 |
| CHEMBL545258 | — | — | 1 | 4.54 |
| CHEMBL542561 | — | — | 1 | 4.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7303 | ARECOLINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL540315 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL541398 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL557795 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL544556 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL537928 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL542065 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL540567 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL545725 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL14 | CARBACHOL | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL543614 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL538467 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL553602 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL538224 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL545258 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL542561 | — | IC50 | = | 31000.0 | nM | 4.51 |