Assay Detail
Functional
CHEMBL2060121
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Agonist activity at human M1 receptor expressed in CHO-K1 cells assessed as calcium mobilization for 6 mins by Calcium4-based staining
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 7.06 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL667 | ACETYLCHOLINE | 4.0 | 1 | 8.96 |
| CHEMBL2059307 | — | — | 1 | 7.92 |
| CHEMBL2059310 | — | — | 1 | 7.70 |
| CHEMBL2059322 | — | — | 1 | 7.36 |
| CHEMBL1242923 | — | — | 1 | 7.21 |
| CHEMBL2059323 | — | — | 1 | 7.18 |
| CHEMBL2059317 | — | — | 1 | 7.17 |
| CHEMBL2059311 | — | — | 1 | 7.14 |
| CHEMBL2059306 | — | — | 1 | 6.96 |
| CHEMBL2059324 | — | — | 1 | 6.96 |
| CHEMBL2059305 | — | — | 1 | 6.80 |
| CHEMBL2059320 | — | — | 1 | 6.52 |
| CHEMBL2059304 | OXIPEROMIDE | 2.0 | 1 | 6.40 |
| CHEMBL2059314 | — | — | 1 | 5.92 |
| CHEMBL2059313 | — | — | 1 | 5.77 |
| CHEMBL2059308 | — | — | 1 | - |
| CHEMBL2059309 | — | — | 1 | - |
| CHEMBL2059312 | — | — | 1 | - |
| CHEMBL2059315 | — | — | 1 | - |
| CHEMBL2059316 | — | — | 1 | - |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | - |
| CHEMBL2059318 | — | — | 1 | - |
| CHEMBL2059319 | — | — | 1 | - |
| CHEMBL2059321 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL667 | ACETYLCHOLINE | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2059307 | — | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2059310 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2059322 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL1242923 | — | EC50 | = | 61.0 | nM | 7.21 |
| CHEMBL2059323 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL2059317 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL2059311 | — | EC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2059306 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2059324 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2059305 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2059320 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2059304 | OXIPEROMIDE | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL2059314 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL2059313 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2059308 | — | EC50 | - | — | - | |
| CHEMBL2059309 | — | EC50 | - | — | - | |
| CHEMBL2059312 | — | EC50 | - | — | - | |
| CHEMBL2059315 | — | EC50 | - | — | - | |
| CHEMBL2059316 | — | EC50 | - | — | - | |
| CHEMBL54 | HALOPERIDOL | EC50 | - | — | - | |
| CHEMBL2059318 | — | EC50 | - | — | - | |
| CHEMBL2059319 | — | EC50 | - | — | - | |
| CHEMBL2059321 | — | EC50 | - | — | - |