Assay Detail
Binding
CHEMBL4825142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human AChE expressed in HEK293 cells by Ellman's method
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Evaluation of γ-carboline-phenothiazine conjugates as simultaneous NMDA receptor blockers and cholinesterase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 5.53 | 9.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3605361 | — | — | 1 | 9.48 |
| CHEMBL807 | MEMANTINE | 4.0 | 1 | 8.31 |
| CHEMBL3605356 | — | — | 1 | 7.10 |
| CHEMBL4855045 | — | — | 1 | 6.29 |
| CHEMBL4850585 | — | — | 1 | 6.27 |
| CHEMBL4873748 | — | — | 1 | 5.96 |
| CHEMBL4849276 | — | — | 1 | 5.72 |
| CHEMBL4850804 | — | — | 1 | 5.66 |
| CHEMBL4870561 | — | — | 1 | 5.66 |
| CHEMBL4848411 | — | — | 1 | 5.64 |
| CHEMBL4874126 | — | — | 1 | 5.58 |
| CHEMBL4878924 | — | — | 1 | 5.28 |
| CHEMBL4864593 | — | — | 1 | 5.21 |
| CHEMBL4860501 | — | — | 1 | 5.11 |
| CHEMBL4850464 | — | — | 1 | 5.07 |
| CHEMBL596112 | — | — | 1 | 5.06 |
| CHEMBL4865927 | — | — | 1 | 5.04 |
| CHEMBL4863376 | — | — | 1 | 4.94 |
| CHEMBL4857977 | — | — | 1 | 4.83 |
| CHEMBL4859070 | — | — | 1 | 4.75 |
| CHEMBL1712867 | — | — | 1 | 4.69 |
| CHEMBL12540 | — | — | 1 | 4.67 |
| CHEMBL4856643 | — | — | 1 | 4.46 |
| CHEMBL261855 | — | — | 1 | 4.45 |
| CHEMBL4846730 | — | — | 1 | 4.30 |
| CHEMBL4849640 | — | — | 1 | 4.28 |
| CHEMBL502 | DONEPEZIL | 4.0 | 1 | - |
| CHEMBL3605369 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3605361 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL807 | MEMANTINE | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3605356 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4855045 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL4850585 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4873748 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4849276 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4850804 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4870561 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4848411 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4874126 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4878924 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4864593 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL4860501 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL4850464 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL596112 | — | IC50 | = | 8700.0 | nM | 5.06 |
| CHEMBL4865927 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL4863376 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4857977 | — | IC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL4859070 | — | IC50 | = | 17600.0 | nM | 4.75 |
| CHEMBL1712867 | — | IC50 | = | 20400.0 | nM | 4.69 |
| CHEMBL12540 | — | IC50 | = | 21400.0 | nM | 4.67 |
| CHEMBL4856643 | — | IC50 | = | 35100.0 | nM | 4.46 |
| CHEMBL261855 | — | IC50 | = | 35400.0 | nM | 4.45 |
| CHEMBL4846730 | — | IC50 | = | 49600.0 | nM | 4.30 |
| CHEMBL4849640 | — | IC50 | = | 52700.0 | nM | 4.28 |
| CHEMBL502 | DONEPEZIL | IC50 | - | — | - | |
| CHEMBL3605369 | — | IC50 | - | — | - |