Assay Detail
Binding
CHEMBL3707954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The assay uses the principle of inhibition of human TMEM27 cleavage by endogenous cellular BACE2 in the Ins1e rat cell line and shedding from the cell surface into the culture medium, followed by detection in an ELISA assay Inhibition of BACE2 prevents the cleavage and shedding in a dose-dependent manner. The stable cell line INS-TMEM27 represents an INS1e-derived cell line with inducible expression (using the TetOn system) of full-length hTMEM27 in a doxycycline-dependent manner. The cells are cultured throughout the experiment in RPMI1640+Glutamax (Invitrogen) Penicillin/Streptomycin, 10% Fetal bovine serum, 100 mM pyruvate, 5 mM beta-mercatptoethanol, 100 micrograms/ml G418 and 100 microgram/ml hygromycin and are grown inadherent culture at 37 C. in a standard CO2 cell culture incubator. INS-TMEM27 cells are seeded in 96-well plates. After 2 days in culture, BACE2 inhibitor is added in a range of concentrations as required by the assay and after a further two hours.
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ins1e |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1,3-oxazines as BACE1 and/or BACE2 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.26 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3680854 | — | — | 1 | 9.00 |
| CHEMBL3680863 | — | — | 1 | 9.00 |
| CHEMBL3680890 | — | — | 1 | 8.40 |
| CHEMBL3680892 | — | — | 1 | 8.22 |
| CHEMBL3680860 | — | — | 1 | 8.22 |
| CHEMBL3680872 | — | — | 1 | 8.15 |
| CHEMBL3680856 | — | — | 1 | 8.15 |
| CHEMBL3680855 | — | — | 1 | 8.10 |
| CHEMBL3680866 | — | — | 1 | 8.05 |
| CHEMBL3680859 | — | — | 1 | 8.00 |
| CHEMBL3680870 | — | — | 1 | 7.70 |
| CHEMBL2347204 | — | — | 1 | 7.68 |
| CHEMBL3680867 | — | — | 1 | 7.64 |
| CHEMBL3680889 | — | — | 1 | 7.64 |
| CHEMBL3680891 | — | — | 1 | 7.51 |
| CHEMBL3680880 | — | — | 1 | 7.46 |
| CHEMBL3680895 | — | — | 1 | 7.21 |
| CHEMBL3680865 | — | — | 1 | 7.19 |
| CHEMBL3680896 | — | — | 1 | 7.19 |
| CHEMBL3680898 | — | — | 1 | 7.17 |
| CHEMBL3680893 | — | — | 1 | 7.13 |
| CHEMBL3680857 | — | — | 1 | 6.97 |
| CHEMBL3639797 | — | — | 1 | 6.96 |
| CHEMBL3680874 | — | — | 1 | 6.91 |
| CHEMBL3680861 | — | — | 1 | 6.91 |
| CHEMBL3680894 | — | — | 1 | 6.85 |
| CHEMBL3680888 | — | — | 1 | 6.65 |
| CHEMBL3680897 | — | — | 1 | 6.57 |
| CHEMBL3680886 | — | — | 1 | 6.29 |
| CHEMBL3680868 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3680854 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3680863 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3680890 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3680892 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3680860 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3680872 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3680856 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3680855 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3680866 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3680859 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3680870 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2347204 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3680867 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3680889 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3680891 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3680880 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3680895 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3680865 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3680896 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3680898 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3680893 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3680857 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3639797 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3680874 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3680861 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL3680894 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3680888 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3680897 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL3680886 | — | IC50 | = | 511.0 | nM | 6.29 |
| CHEMBL3680868 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL3680879 | — | IC50 | = | 709.0 | nM | 6.15 |
| CHEMBL2347205 | — | IC50 | = | 1174.0 | nM | 5.93 |
| CHEMBL3680878 | — | IC50 | = | 1405.0 | nM | 5.85 |
| CHEMBL3680869 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3680887 | — | IC50 | = | 4029.0 | nM | 5.39 |