Assay Detail
Binding
CHEMBL744383
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of specific [3H](R)-QNB binding to Muscarinic acetylcholine receptor in rat brain membranes
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Brain membranes |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and biological characterization of 1,4,5,6-tetrahydropyrimidine and 2-amino-3,4,5,6-tetrahydropyridine derivatives as selective m1 agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.18 | 6.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20835 | ACECLIDINE | 3.0 | 1 | 6.29 |
| CHEMBL7303 | ARECOLINE | -1.0 | 1 | 6.00 |
| CHEMBL416736 | — | — | 1 | 6.00 |
| CHEMBL282909 | — | — | 1 | 5.85 |
| CHEMBL543030 | — | — | 1 | 5.82 |
| CHEMBL541398 | — | — | 1 | 5.66 |
| CHEMBL21284 | — | — | 1 | 5.64 |
| CHEMBL21530 | — | — | 1 | 5.58 |
| CHEMBL277014 | — | — | 1 | 5.57 |
| CHEMBL537928 | — | — | 1 | 5.48 |
| CHEMBL542065 | — | — | 1 | 5.48 |
| CHEMBL22089 | — | — | 1 | 5.40 |
| CHEMBL543031 | — | — | 1 | 5.39 |
| CHEMBL281411 | — | — | 1 | 5.29 |
| CHEMBL279295 | — | — | 1 | 5.29 |
| CHEMBL21733 | — | — | 1 | 5.28 |
| CHEMBL14 | CARBACHOL | 4.0 | 1 | 5.26 |
| CHEMBL21565 | — | — | 1 | 5.21 |
| CHEMBL550 | PILOCARPINE | 4.0 | 1 | 5.12 |
| CHEMBL538467 | — | — | 1 | 5.04 |
| CHEMBL538982 | — | — | 1 | 5.03 |
| CHEMBL545376 | — | — | 1 | 4.92 |
| CHEMBL542064 | — | — | 1 | 4.89 |
| CHEMBL542559 | — | — | 1 | 4.85 |
| CHEMBL554855 | — | — | 1 | 4.85 |
| CHEMBL542560 | — | — | 1 | 4.82 |
| CHEMBL279895 | — | — | 1 | 4.80 |
| CHEMBL545386 | — | — | 1 | 4.68 |
| CHEMBL21496 | — | — | 1 | 4.50 |
| CHEMBL542315 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20835 | ACECLIDINE | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL7303 | ARECOLINE | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL416736 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL282909 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL543030 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL541398 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL21284 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL21530 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL277014 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL537928 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL542065 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL22089 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL543031 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL281411 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL279295 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL21733 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL14 | CARBACHOL | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL21565 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL550 | PILOCARPINE | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL538467 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL538982 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL545376 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL542064 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL542559 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL554855 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL542560 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL279895 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL545386 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL21496 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL542315 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL555850 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL545611 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL545148 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL276994 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL539234 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL21322 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL553883 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL21779 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL21402 | — | IC50 | > | 100000.0 | nM | - |