Assay Detail
Binding
CHEMBL2398915
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Inhibition of partially purified human gamma-secretase-mediated cleavage of notch fusion protein measured after overnight incubation by ELISA
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.88 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | 2.0 | 1 | 8.82 |
| CHEMBL2396772 | — | — | 1 | 8.77 |
| CHEMBL2396771 | — | — | 1 | 8.77 |
| CHEMBL2396770 | — | — | 1 | 8.57 |
| CHEMBL520733 | SEMAGACESTAT | 3.0 | 1 | 8.49 |
| CHEMBL1089001 | ENT A | — | 1 | 8.33 |
| CHEMBL2396778 | — | — | 1 | 8.18 |
| CHEMBL2396777 | — | — | 1 | 8.02 |
| CHEMBL463981 | BEGACESTAT | 2.0 | 1 | 7.96 |
| CHEMBL571818 | — | — | 1 | 7.85 |
| CHEMBL2396779 | — | — | 1 | 7.77 |
| CHEMBL1093101 | — | — | 1 | 7.54 |
| CHEMBL2396776 | — | — | 1 | 7.38 |
| CHEMBL2396775 | — | — | 1 | 7.37 |
| CHEMBL2396773 | — | — | 1 | 6.80 |
| CHEMBL2396774 | — | — | 1 | 6.66 |
| CHEMBL570016 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090771 | AVAGACESTAT | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2396772 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2396771 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2396770 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL520733 | SEMAGACESTAT | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1089001 | ENT A | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL2396778 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2396777 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL463981 | BEGACESTAT | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL571818 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2396779 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1093101 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2396776 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2396775 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2396773 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2396774 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL570016 | — | IC50 | = | 250.0 | nM | 6.60 |