Assay Detail
Binding
CHEMBL4183116
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BACE1 in human H4 cells transfected with wild type APP assessed as reduction in soluble portion of APPbeta level in cells incubated for overnight by ELISA
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.92 | 10.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3922902 | — | — | 1 | 10.85 |
| CHEMBL4212046 | — | — | 1 | 10.48 |
| CHEMBL4217023 | — | — | 1 | 10.47 |
| CHEMBL4203860 | — | — | 1 | 9.96 |
| CHEMBL4215837 | — | — | 1 | 9.19 |
| CHEMBL3972449 | — | — | 1 | 8.54 |
| CHEMBL3967984 | — | — | 1 | 8.42 |
| CHEMBL4211913 | — | — | 1 | 8.41 |
| CHEMBL3917530 | — | — | 1 | 8.32 |
| CHEMBL3952064 | — | — | 1 | 8.29 |
| CHEMBL4204163 | — | — | 1 | 8.14 |
| CHEMBL3947194 | — | — | 1 | 7.90 |
| CHEMBL3979124 | — | — | 1 | 7.62 |
| CHEMBL3983988 | — | — | 1 | 7.57 |
| CHEMBL4205912 | — | — | 1 | 7.42 |
| CHEMBL3414707 | — | — | 1 | 7.41 |
| CHEMBL3941301 | — | — | 1 | 7.32 |
| CHEMBL4204215 | — | — | 1 | 6.96 |
| CHEMBL4203347 | — | — | 1 | 6.77 |
| CHEMBL4214603 | — | — | 1 | 6.60 |
| CHEMBL4207711 | — | — | 1 | 6.09 |
| CHEMBL4209354 | — | — | 1 | 6.07 |
| CHEMBL4214785 | — | — | 1 | 5.69 |
| CHEMBL4209994 | — | — | 1 | 5.54 |
| CHEMBL3672916 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3922902 | — | IC50 | = | 0.014 | nM | 10.85 |
| CHEMBL4212046 | — | IC50 | = | 0.033 | nM | 10.48 |
| CHEMBL4217023 | — | IC50 | = | 0.034 | nM | 10.47 |
| CHEMBL4203860 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4215837 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL3972449 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3967984 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4211913 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3917530 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3952064 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4204163 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3947194 | — | IC50 | = | 12.5 | nM | 7.90 |
| CHEMBL3979124 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL3983988 | — | IC50 | = | 26.9 | nM | 7.57 |
| CHEMBL4205912 | — | IC50 | = | 38.4 | nM | 7.42 |
| CHEMBL3414707 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3941301 | — | IC50 | = | 47.6 | nM | 7.32 |
| CHEMBL4204215 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4203347 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4214603 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4207711 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4209354 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL4214785 | — | IC50 | = | 2050.0 | nM | 5.69 |
| CHEMBL4209994 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL3672916 | — | IC50 | < | 0.54 | nM | - |