Assay Detail
Binding
CHEMBL752412
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Binding affinity towards cloned human muscarinic acetylcholine receptor M3 stably expressed in CHO-K1 cells using [3H]N-methylscopolamine
36
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO-K1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 5.93 | 7.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL423831 | — | — | 1 | 7.59 |
| CHEMBL434684 | — | — | 1 | 7.50 |
| CHEMBL171102 | — | — | 1 | 7.17 |
| CHEMBL167223 | — | — | 1 | 7.02 |
| CHEMBL1493369 | — | — | 1 | 6.86 |
| CHEMBL353290 | — | — | 1 | 6.58 |
| CHEMBL354523 | — | — | 1 | 6.55 |
| CHEMBL170221 | — | — | 1 | 6.54 |
| CHEMBL354678 | — | — | 1 | 6.51 |
| CHEMBL354841 | — | — | 1 | 6.30 |
| CHEMBL168707 | — | — | 1 | 6.30 |
| CHEMBL169401 | — | — | 1 | 6.24 |
| CHEMBL170088 | — | — | 1 | 6.20 |
| CHEMBL172233 | — | — | 1 | 6.15 |
| CHEMBL171216 | — | — | 1 | 6.13 |
| CHEMBL168704 | — | — | 1 | 6.02 |
| CHEMBL352723 | — | — | 1 | 5.98 |
| CHEMBL167027 | — | — | 1 | 5.93 |
| CHEMBL169494 | — | — | 1 | 5.81 |
| CHEMBL355392 | — | — | 1 | 5.75 |
| CHEMBL355769 | — | — | 1 | 5.74 |
| CHEMBL355455 | — | — | 1 | 5.72 |
| CHEMBL352375 | — | — | 3 | 5.65 |
| CHEMBL352966 | — | — | 1 | 5.60 |
| CHEMBL369575 | — | — | 1 | 5.56 |
| CHEMBL352404 | — | — | 1 | 5.50 |
| CHEMBL564226 | (S)-(+)-DIMETHINDENE | — | 1 | 5.47 |
| CHEMBL355560 | — | — | 1 | 5.09 |
| CHEMBL169594 | — | — | 1 | 5.09 |
| CHEMBL172234 | — | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL423831 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL434684 | — | Ki | = | 31.62 | nM | 7.50 |
| CHEMBL171102 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL167223 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL1493369 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL353290 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL354523 | — | Ki | = | 281.84 | nM | 6.55 |
| CHEMBL170221 | — | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL354678 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL354841 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL168707 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL169401 | — | Ki | = | 575.44 | nM | 6.24 |
| CHEMBL170088 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL172233 | — | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL171216 | — | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL168704 | — | Ki | = | 954.99 | nM | 6.02 |
| CHEMBL352723 | — | Ki | = | 1047.13 | nM | 5.98 |
| CHEMBL167027 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL169494 | — | Ki | = | 1548.82 | nM | 5.81 |
| CHEMBL355392 | — | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL355769 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL355455 | — | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL352375 | — | Ki | = | 2238.72 | nM | 5.65 |
| CHEMBL352966 | — | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL369575 | — | Ki | = | 2754.23 | nM | 5.56 |
| CHEMBL352404 | — | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL564226 | (S)-(+)-DIMETHINDENE | Ki | = | 3388.44 | nM | 5.47 |
| CHEMBL352375 | — | Ki | = | 4073.8 | nM | 5.39 |
| CHEMBL169594 | — | Ki | = | 8128.31 | nM | 5.09 |
| CHEMBL355560 | — | Ki | = | 8128.31 | nM | 5.09 |
| CHEMBL172234 | — | Ki | = | 8912.51 | nM | 5.05 |
| CHEMBL169680 | — | Ki | = | 11748.98 | nM | 4.93 |
| CHEMBL352375 | — | Ki | = | 20892.96 | nM | 4.68 |
| CHEMBL352779 | — | Ki | = | 23988.33 | nM | 4.62 |
| CHEMBL355851 | — | Ki | = | 48977.88 | nM | 4.31 |
| CHEMBL168223 | — | Ki | = | 134896.29 | nM | - |