Assay Detail
Binding
CHEMBL887940
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma secretase assessed as reduction of amyloid beta level in H4 cells
29
Total Activities
29
Compounds Tested
1
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
Discovery of (S)-2-((S)-2-(3,5-difluorophenyl)-2-hydroxyacetamido)-N-((S,Z)-3-methyl-4-oxo-4,5-dihydro-3H-benzo[d][1,2]diazepin-5-yl)propanamide (BMS-433796): a gamma-secretase inhibitor with Abeta lowering activity in a transgenic mouse model of Alzheimer's disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.18 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392246 | — | — | 1 | 9.70 |
| CHEMBL247361 | — | — | 1 | 9.52 |
| CHEMBL397844 | — | — | 1 | 9.40 |
| CHEMBL396808 | — | — | 1 | 9.30 |
| CHEMBL247155 | — | — | 1 | 9.15 |
| CHEMBL439210 | — | — | 1 | 9.00 |
| CHEMBL429292 | — | — | 1 | 9.00 |
| CHEMBL246785 | — | — | 1 | 8.89 |
| CHEMBL397394 | — | — | 1 | 8.72 |
| CHEMBL245385 | — | — | 1 | 8.70 |
| CHEMBL397335 | — | — | 1 | 8.70 |
| CHEMBL246575 | — | — | 1 | 8.52 |
| CHEMBL246784 | — | — | 1 | 8.40 |
| CHEMBL246369 | — | — | 1 | 8.22 |
| CHEMBL397547 | — | — | 1 | 8.10 |
| CHEMBL436997 | — | — | 1 | 8.05 |
| CHEMBL247560 | — | — | 1 | 8.00 |
| CHEMBL397548 | — | — | 1 | 8.00 |
| CHEMBL247154 | — | — | 1 | 7.85 |
| CHEMBL247360 | — | — | 1 | 7.85 |
| CHEMBL396164 | — | — | 1 | 7.66 |
| CHEMBL265897 | — | — | 1 | 7.62 |
| CHEMBL396639 | — | — | 1 | 7.52 |
| CHEMBL246573 | — | — | 1 | 7.37 |
| CHEMBL397843 | — | — | 1 | 7.25 |
| CHEMBL246370 | — | — | 1 | 7.23 |
| CHEMBL246371 | — | — | 1 | 6.79 |
| CHEMBL395198 | — | — | 1 | 6.57 |
| CHEMBL393484 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392246 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL247361 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL397844 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL396808 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL247155 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL439210 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL429292 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL246785 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL397394 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL245385 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL397335 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL246575 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL246784 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL246369 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL397547 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL436997 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL247560 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL397548 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL247154 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL247360 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL396164 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL265897 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL396639 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL246573 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL397843 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL246370 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL246371 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL395198 | — | IC50 | = | 269.0 | nM | 6.57 |
| CHEMBL393484 | — | IC50 | = | 750.0 | nM | 6.12 |