Assay Detail
ADMET
CHEMBL4183128
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Inhibition of human BACE2 using biotin-GLTNIKTEEISEISYEVEFR-C[Oregon green]KK-OH as substrate after 3 hrs by fluorescence polarization assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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 | 13 | 7.04 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215837 | — | — | 1 | 8.41 |
| CHEMBL3672916 | — | — | 1 | 8.35 |
| CHEMBL3967984 | — | — | 1 | 7.67 |
| CHEMBL3983988 | — | — | 1 | 7.41 |
| CHEMBL4205912 | — | — | 1 | 7.37 |
| CHEMBL4211913 | — | — | 1 | 7.22 |
| CHEMBL3972449 | — | — | 1 | 7.15 |
| CHEMBL3979124 | — | — | 1 | 6.63 |
| CHEMBL3952064 | — | — | 1 | 6.62 |
| CHEMBL3917530 | — | — | 1 | 6.47 |
| CHEMBL4204163 | — | — | 1 | 6.43 |
| CHEMBL3947194 | — | — | 1 | 5.97 |
| CHEMBL3941301 | — | — | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215837 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3672916 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL3967984 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL3983988 | — | IC50 | = | 38.9 | nM | 7.41 |
| CHEMBL4205912 | — | IC50 | = | 42.9 | nM | 7.37 |
| CHEMBL4211913 | — | IC50 | = | 60.7 | nM | 7.22 |
| CHEMBL3972449 | — | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL3979124 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL3952064 | — | IC50 | = | 238.0 | nM | 6.62 |
| CHEMBL3917530 | — | IC50 | = | 338.0 | nM | 6.47 |
| CHEMBL4204163 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL3947194 | — | IC50 | = | 1072.0 | nM | 5.97 |
| CHEMBL3941301 | — | IC50 | = | 1709.0 | nM | 5.77 |