Assay Detail
Functional
CHEMBL938553
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Agonist activity at muscarinic M1 receptor
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 21 | 5.67 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522460 | — | — | 1 | 6.54 |
| CHEMBL478662 | — | — | 1 | 6.48 |
| CHEMBL513765 | — | — | 1 | 6.29 |
| CHEMBL471213 | — | — | 1 | 6.06 |
| CHEMBL511833 | — | — | 1 | 6.04 |
| CHEMBL487557 | — | — | 1 | 6.03 |
| CHEMBL487762 | — | — | 1 | 5.85 |
| CHEMBL471636 | — | — | 1 | 5.68 |
| CHEMBL485913 | — | — | 1 | 5.68 |
| CHEMBL485755 | — | — | 1 | 5.64 |
| CHEMBL486758 | — | — | 1 | 5.58 |
| CHEMBL471635 | — | — | 1 | 5.57 |
| CHEMBL485953 | — | — | 1 | 5.48 |
| CHEMBL487986 | — | — | 1 | 5.44 |
| CHEMBL521030 | — | — | 1 | 5.39 |
| CHEMBL487984 | — | — | 1 | 5.36 |
| CHEMBL486331 | — | — | 1 | 5.19 |
| CHEMBL487558 | — | — | 1 | 5.15 |
| CHEMBL487985 | — | — | 1 | 5.02 |
| CHEMBL521388 | — | — | 1 | 4.96 |
| CHEMBL487788 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522460 | — | EC50 | = | 289.0 | nM | 6.54 |
| CHEMBL478662 | — | EC50 | = | 334.0 | nM | 6.48 |
| CHEMBL513765 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL471213 | — | EC50 | = | 880.0 | nM | 6.06 |
| CHEMBL511833 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL487557 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL487762 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL471636 | — | EC50 | = | 2110.0 | nM | 5.68 |
| CHEMBL485913 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL485755 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL486758 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL471635 | — | EC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL485953 | — | EC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL487986 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL521030 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL487984 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL486331 | — | EC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL487558 | — | EC50 | = | 7110.0 | nM | 5.15 |
| CHEMBL487985 | — | EC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL521388 | — | EC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL487788 | — | EC50 | > | 10000.0 | nM | - |