Assay Detail
Binding
CHEMBL2060673
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of gamma secretase-mediated amyloid beta42 production in human H4 cells expressing human APP swedish mutant
21
Total Activities
20
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
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 8.19 | 9.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2059813 | — | — | 1 | 9.75 |
| CHEMBL1090771 | AVAGACESTAT | 2.0 | 1 | 9.65 |
| CHEMBL2059021 | — | — | 1 | 9.00 |
| CHEMBL2059814 | — | — | 1 | 8.98 |
| CHEMBL2059815 | — | — | 1 | 8.75 |
| CHEMBL2059016 | — | — | 2 | 8.56 |
| CHEMBL2059011 | — | — | 1 | 8.32 |
| CHEMBL2059819 | — | — | 1 | 8.16 |
| CHEMBL2059014 | — | — | 1 | 8.13 |
| CHEMBL2059015 | — | — | 1 | 8.02 |
| CHEMBL2059818 | — | — | 1 | 7.96 |
| CHEMBL2059018 | — | — | 1 | 7.92 |
| CHEMBL2059020 | — | — | 1 | 7.91 |
| CHEMBL2059820 | — | — | 1 | 7.83 |
| CHEMBL2059012 | — | — | 1 | 7.79 |
| CHEMBL2059816 | — | — | 1 | 7.65 |
| CHEMBL2059017 | — | — | 1 | 7.61 |
| CHEMBL2059019 | — | — | 1 | 7.34 |
| CHEMBL2059013 | — | — | 1 | 7.23 |
| CHEMBL2059817 | — | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2059813 | — | IC50 | = | 0.178 | nM | 9.75 |
| CHEMBL1090771 | AVAGACESTAT | IC50 | = | 0.225 | nM | 9.65 |
| CHEMBL2059021 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL2059814 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL2059815 | — | IC50 | = | 1.77 | nM | 8.75 |
| CHEMBL2059016 | — | IC50 | = | 2.75 | nM | 8.56 |
| CHEMBL2059016 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL2059011 | — | IC50 | = | 4.77 | nM | 8.32 |
| CHEMBL2059819 | — | IC50 | = | 6.92 | nM | 8.16 |
| CHEMBL2059014 | — | IC50 | = | 7.47 | nM | 8.13 |
| CHEMBL2059015 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL2059818 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL2059018 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL2059020 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL2059820 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL2059012 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL2059816 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL2059017 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL2059019 | — | IC50 | = | 45.5 | nM | 7.34 |
| CHEMBL2059013 | — | IC50 | = | 58.7 | nM | 7.23 |
| CHEMBL2059817 | — | IC50 | = | 87.1 | nM | 7.06 |