Assay Detail
Binding
CHEMBL4815609
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-NMS from human muscarinic M1 receptor expressed in CHO cell membranes assessed as inhibition constant by radioligand competition analysis
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dibenzodiazepinone-type muscarinic receptor antagonists conjugated to basic peptides: Impact of the linker moiety and unnatural amino acids on M<sub>2</sub>R selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 76 | 7.19 | 9.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4851514 | — | — | 1 | 9.32 |
| CHEMBL4870127 | — | — | 1 | 9.16 |
| CHEMBL4864987 | — | — | 1 | 9.14 |
| CHEMBL4847898 | — | — | 1 | 9.07 |
| CHEMBL4862735 | — | — | 1 | 9.04 |
| CHEMBL4871700 | — | — | 1 | 9.03 |
| CHEMBL4855492 | — | — | 1 | 9.02 |
| CHEMBL4871153 | — | — | 1 | 8.94 |
| CHEMBL4876725 | — | — | 1 | 8.94 |
| CHEMBL4874955 | — | — | 1 | 8.90 |
| CHEMBL4856113 | — | — | 1 | 8.90 |
| CHEMBL4861252 | — | — | 1 | 8.89 |
| CHEMBL4864727 | — | — | 1 | 8.87 |
| CHEMBL4859378 | — | — | 1 | 8.82 |
| CHEMBL4852186 | — | — | 1 | 8.70 |
| CHEMBL4597498 | — | — | 1 | 8.60 |
| CHEMBL4878646 | — | — | 1 | 8.59 |
| CHEMBL4876453 | — | — | 1 | 8.42 |
| CHEMBL4878717 | — | — | 1 | 8.41 |
| CHEMBL295388 | — | — | 1 | 8.40 |
| CHEMBL4848683 | — | — | 1 | 8.19 |
| CHEMBL4872608 | — | — | 1 | 8.17 |
| CHEMBL4852646 | — | — | 1 | 8.15 |
| CHEMBL4858398 | — | — | 1 | 8.11 |
| CHEMBL4059733 | — | — | 1 | 8.10 |
| CHEMBL4852868 | — | — | 1 | 8.09 |
| CHEMBL4863285 | — | — | 1 | 8.04 |
| CHEMBL4850130 | — | — | 1 | 7.93 |
| CHEMBL4856659 | — | — | 1 | 7.79 |
| CHEMBL4862996 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4851514 | — | Ki | = | 0.4786 | nM | 9.32 |
| CHEMBL4870127 | — | Ki | = | 0.6918 | nM | 9.16 |
| CHEMBL4864987 | — | Ki | = | 0.7244 | nM | 9.14 |
| CHEMBL4847898 | — | Ki | = | 0.8511 | nM | 9.07 |
| CHEMBL4862735 | — | Ki | = | 0.912 | nM | 9.04 |
| CHEMBL4871700 | — | Ki | = | 0.9333 | nM | 9.03 |
| CHEMBL4855492 | — | Ki | = | 0.955 | nM | 9.02 |
| CHEMBL4871153 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL4876725 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL4874955 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL4856113 | — | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL4861252 | — | Ki | = | 1.288 | nM | 8.89 |
| CHEMBL4864727 | — | Ki | = | 1.349 | nM | 8.87 |
| CHEMBL4859378 | — | Ki | = | 1.514 | nM | 8.82 |
| CHEMBL4852186 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL4597498 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL4878646 | — | Ki | = | 2.57 | nM | 8.59 |
| CHEMBL4876453 | — | Ki | = | 3.802 | nM | 8.42 |
| CHEMBL4878717 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL295388 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL4848683 | — | Ki | = | 6.457 | nM | 8.19 |
| CHEMBL4872608 | — | Ki | = | 6.761 | nM | 8.17 |
| CHEMBL4852646 | — | Ki | = | 7.079 | nM | 8.15 |
| CHEMBL4858398 | — | Ki | = | 7.762 | nM | 8.11 |
| CHEMBL4059733 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL4852868 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL4863285 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL4850130 | — | Ki | = | 11.75 | nM | 7.93 |
| CHEMBL4856659 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL4862996 | — | Ki | = | 19.05 | nM | 7.72 |
| CHEMBL4846562 | — | Ki | = | 21.38 | nM | 7.67 |
| CHEMBL4854886 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL4872720 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL4846958 | — | Ki | = | 38.9 | nM | 7.41 |
| CHEMBL4596065 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4862087 | — | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL4857722 | — | Ki | = | 46.77 | nM | 7.33 |
| CHEMBL4851265 | — | Ki | = | 51.29 | nM | 7.29 |
| CHEMBL4873621 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL4865939 | — | Ki | = | 53.7 | nM | 7.27 |
| CHEMBL4862098 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL4869723 | — | Ki | = | 61.66 | nM | 7.21 |
| CHEMBL4867301 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL4867483 | — | Ki | = | 87.1 | nM | 7.06 |
| CHEMBL4596899 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4861655 | — | Ki | = | 141.25 | nM | 6.85 |
| CHEMBL4863723 | — | Ki | = | 154.88 | nM | 6.81 |
| CHEMBL4873979 | — | Ki | = | 223.87 | nM | 6.65 |
| CHEMBL4870729 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL4850553 | — | Ki | = | 281.84 | nM | 6.55 |