Assay Detail
Binding
CHEMBL5029741
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Inhibition of BACE2 (unknown origin) using APP harboring Swedish Lys-Met/Asn-Leu mutant-derived peptide as substrate incubated for 2 hrs by FRET assay
15
Total Activities
15
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
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.74 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5074719 | — | — | 1 | 8.51 |
| CHEMBL5081571 | — | — | 1 | 7.80 |
| CHEMBL5093088 | — | — | 1 | 7.73 |
| CHEMBL5084928 | — | — | 1 | 7.33 |
| CHEMBL5091877 | — | — | 1 | 7.18 |
| CHEMBL5090362 | — | — | 1 | 6.83 |
| CHEMBL5082356 | — | — | 1 | 6.72 |
| CHEMBL5092328 | — | — | 1 | 6.71 |
| CHEMBL5074678 | — | — | 1 | 6.47 |
| CHEMBL5083750 | — | — | 1 | 6.39 |
| CHEMBL5089679 | — | — | 1 | 6.33 |
| CHEMBL5075689 | — | — | 1 | 6.32 |
| CHEMBL5075795 | — | — | 1 | 5.94 |
| CHEMBL4465534 | — | — | 1 | 5.68 |
| CHEMBL5088971 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074719 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5081571 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5093088 | — | IC50 | = | 18.6 | nM | 7.73 |
| CHEMBL5084928 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5091877 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5090362 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL5082356 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL5092328 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL5074678 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5083750 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL5089679 | — | IC50 | = | 468.0 | nM | 6.33 |
| CHEMBL5075689 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL5075795 | — | IC50 | = | 1148.0 | nM | 5.94 |
| CHEMBL4465534 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5088971 | — | IC50 | = | 6700.0 | nM | 5.17 |