Assay Detail
Binding
CHEMBL4183113
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Inhibition of human BACE1 using biotin-GLTNIKTEEISEISYEVEFR-C[Oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization assay
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 | 6.55 | 8.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215837 | — | — | 1 | 8.03 |
| CHEMBL4211913 | — | — | 1 | 7.66 |
| CHEMBL3972449 | — | — | 1 | 7.64 |
| CHEMBL3967984 | — | — | 1 | 7.54 |
| CHEMBL3952064 | — | — | 1 | 7.43 |
| CHEMBL4205912 | — | — | 1 | 7.38 |
| CHEMBL3917530 | — | — | 1 | 7.22 |
| CHEMBL4204163 | — | — | 1 | 7.14 |
| CHEMBL3947194 | — | — | 1 | 6.97 |
| CHEMBL4212046 | — | — | 1 | 6.96 |
| CHEMBL3983988 | — | — | 1 | 6.75 |
| CHEMBL3979124 | — | — | 1 | 6.64 |
| CHEMBL3922902 | — | — | 1 | 6.58 |
| CHEMBL4203860 | — | — | 1 | 6.57 |
| CHEMBL3941301 | — | — | 1 | 6.27 |
| CHEMBL3414707 | — | — | 1 | 6.15 |
| CHEMBL4217023 | — | — | 1 | 6.00 |
| CHEMBL4207711 | — | — | 1 | 5.88 |
| CHEMBL4204215 | — | — | 1 | 5.72 |
| CHEMBL4203347 | — | — | 1 | 5.29 |
| CHEMBL4209354 | — | — | 1 | 5.22 |
| CHEMBL4214603 | — | — | 1 | 5.04 |
| CHEMBL4214785 | — | — | 1 | 4.62 |
| CHEMBL3672916 | — | — | 1 | - |
| CHEMBL4209994 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215837 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4211913 | — | IC50 | = | 21.8 | nM | 7.66 |
| CHEMBL3972449 | — | IC50 | = | 22.8 | nM | 7.64 |
| CHEMBL3967984 | — | IC50 | = | 29.1 | nM | 7.54 |
| CHEMBL3952064 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL4205912 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3917530 | — | IC50 | = | 60.2 | nM | 7.22 |
| CHEMBL4204163 | — | IC50 | = | 72.5 | nM | 7.14 |
| CHEMBL3947194 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4212046 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3983988 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL3979124 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL3922902 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4203860 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3941301 | — | IC50 | = | 536.0 | nM | 6.27 |
| CHEMBL3414707 | — | IC50 | = | 704.0 | nM | 6.15 |
| CHEMBL4217023 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4207711 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4204215 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL4203347 | — | IC50 | = | 5170.0 | nM | 5.29 |
| CHEMBL4209354 | — | IC50 | = | 6060.0 | nM | 5.22 |
| CHEMBL4214603 | — | IC50 | = | 9160.0 | nM | 5.04 |
| CHEMBL4214785 | — | IC50 | = | 23900.0 | nM | 4.62 |
| CHEMBL3672916 | — | IC50 | < | 2.2 | nM | - |
| CHEMBL4209994 | — | IC50 | > | 79300.0 | nM | - |