Assay Detail
Binding
CHEMBL1816006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Modulation of gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in amyloid beta42 production after 20 to 24 hrs by liquid phase electrochemiluminescence assay
38
Total Activities
37
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | H4 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
NSAID-derived γ-secretase modulation requires an acidic moiety on the carbazole scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 4.56 | 5.54 |
| EC50 | 11 | 4.65 | 4.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218756 | — | — | 1 | 5.54 |
| CHEMBL1812400 | — | — | 1 | 4.92 |
| CHEMBL1812426 | — | — | 2 | 4.89 |
| CHEMBL1812421 | — | — | 1 | 4.82 |
| CHEMBL1812424 | — | — | 1 | 4.72 |
| CHEMBL1812422 | — | — | 1 | 4.68 |
| CHEMBL1812397 | — | — | 1 | 4.68 |
| CHEMBL1812408 | — | — | 1 | 4.62 |
| CHEMBL1812423 | — | — | 1 | 4.57 |
| CHEMBL1812407 | — | — | 1 | 4.55 |
| CHEMBL1812428 | — | — | 1 | 4.51 |
| CHEMBL1812398 | — | — | 1 | 4.50 |
| CHEMBL1812416 | — | — | 1 | 4.50 |
| CHEMBL1812406 | — | — | 1 | 4.43 |
| CHEMBL1812405 | — | — | 1 | 4.42 |
| CHEMBL1812429 | — | — | 1 | 4.31 |
| CHEMBL1812396 | — | — | 1 | 4.30 |
| CHEMBL1812418 | — | — | 1 | 4.10 |
| CHEMBL1812427 | — | — | 1 | 4.05 |
| CHEMBL1812425 | — | — | 1 | - |
| CHEMBL247691 | — | — | 1 | - |
| CHEMBL1812417 | — | — | 1 | - |
| CHEMBL1812419 | — | — | 1 | - |
| CHEMBL1812415 | — | — | 1 | - |
| CHEMBL1812414 | — | — | 1 | - |
| CHEMBL1812413 | — | — | 1 | - |
| CHEMBL1812412 | — | — | 1 | - |
| CHEMBL1812420 | — | — | 1 | - |
| CHEMBL1812401 | — | — | 1 | - |
| CHEMBL1812411 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218756 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL1812400 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1812426 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1812426 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL1812421 | — | EC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL1812424 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL1812422 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1812397 | — | EC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1812408 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL1812423 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL1812407 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL1812428 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL1812398 | — | EC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL1812416 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL1812406 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL1812405 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL1812429 | — | EC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL1812396 | — | EC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL1812418 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL1812427 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL1812399 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812401 | — | IC50 | > | 35000.0 | nM | - |
| CHEMBL1812402 | — | IC50 | = | 252000.0 | nM | - |
| CHEMBL1812403 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812404 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL375635 | — | IC50 | > | 6900.0 | nM | - |
| CHEMBL1812409 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1812410 | — | IC50 | = | 113000.0 | nM | - |
| CHEMBL1812411 | — | EC50 | > | 80000.0 | nM | - |
| CHEMBL1812419 | — | IC50 | = | 104000.0 | nM | - |
| CHEMBL1812420 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812412 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1812425 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812413 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL247691 | — | IC50 | > | 19000.0 | nM | - |
| CHEMBL1812414 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812415 | — | IC50 | > | 80000.0 | nM | - |
| CHEMBL1812417 | — | IC50 | > | 80000.0 | nM | - |