Assay Detail
Binding
CHEMBL997193
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Inhibition of gamma secretase in human SH-SY5Y cells by HTRF assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SH-SY5Y |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Novel orally bioavailable gamma-secretase inhibitors with excellent in vivo activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.75 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL468083 | — | — | 1 | 10.52 |
| CHEMBL467457 | — | — | 1 | 10.22 |
| CHEMBL523832 | — | — | 1 | 10.22 |
| CHEMBL512282 | — | — | 1 | 10.22 |
| CHEMBL495009 | — | — | 1 | 10.22 |
| CHEMBL511572 | — | — | 1 | 10.15 |
| CHEMBL495185 | — | — | 1 | 10.10 |
| CHEMBL523883 | — | — | 1 | 9.92 |
| CHEMBL511928 | — | — | 1 | 9.82 |
| CHEMBL494588 | — | — | 1 | 9.77 |
| CHEMBL511375 | — | — | 1 | 9.68 |
| CHEMBL196215 | — | — | 1 | 9.62 |
| CHEMBL506323 | — | — | 1 | 9.47 |
| CHEMBL466421 | — | — | 1 | 9.39 |
| CHEMBL466256 | — | — | 1 | 9.38 |
| CHEMBL513674 | — | — | 1 | 9.38 |
| CHEMBL512596 | — | — | 1 | 9.34 |
| CHEMBL494769 | — | — | 1 | 9.09 |
| CHEMBL492394 | — | — | 1 | 8.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL468083 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL467457 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL523832 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL512282 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL495009 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL511572 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL495185 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL523883 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL511928 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL494588 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL511375 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL196215 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL506323 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL466421 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL466256 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL513674 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL512596 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL494769 | — | IC50 | = | 0.82 | nM | 9.09 |
| CHEMBL492394 | — | IC50 | = | 1.65 | nM | 8.78 |