Assay Detail
ADMET
CHEMBL4183135
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Displacement of [3H]-PF-6475886 from recombinant human full length Myc-DDK-tagged BACE2 expressed in HEK293 cell membranes after 30 mins by parallel scintillation proximity assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 5 | 7.58 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3672916 | — | — | 1 | 8.48 |
| CHEMBL4205912 | — | — | 1 | 7.75 |
| CHEMBL3967984 | — | — | 1 | 7.70 |
| CHEMBL3972449 | — | — | 1 | 7.24 |
| CHEMBL3952064 | — | — | 1 | 6.71 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3672916 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4205912 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL3967984 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3972449 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3952064 | — | IC50 | = | 194.0 | nM | 6.71 |