Assay Detail
Binding
CHEMBL1024504
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BACE1 in human HEK293 cells overexpressing APP with Swedish mutation assessed as inhibition of amyloid beta 40 production
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 59 | 6.81 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539973 | — | — | 1 | 7.92 |
| CHEMBL538636 | — | — | 1 | 7.72 |
| CHEMBL540729 | — | — | 1 | 7.57 |
| CHEMBL553571 | — | — | 1 | 7.52 |
| CHEMBL552743 | — | — | 1 | 7.47 |
| CHEMBL555517 | — | — | 1 | 7.38 |
| CHEMBL539466 | — | — | 1 | 7.35 |
| CHEMBL553612 | — | — | 1 | 7.28 |
| CHEMBL539465 | — | — | 1 | 7.28 |
| CHEMBL538637 | — | — | 1 | 7.14 |
| CHEMBL221597 | — | — | 1 | 7.10 |
| CHEMBL551980 | — | — | 1 | 7.10 |
| CHEMBL563604 | — | — | 1 | 7.10 |
| CHEMBL558938 | — | — | 1 | 7.09 |
| CHEMBL539975 | — | — | 1 | 7.07 |
| CHEMBL555916 | — | — | 1 | 7.06 |
| CHEMBL553458 | — | — | 1 | 7.04 |
| CHEMBL553457 | — | — | 1 | 7.04 |
| CHEMBL541976 | — | — | 1 | 7.04 |
| CHEMBL557554 | — | — | 1 | 7.03 |
| CHEMBL557352 | — | — | 1 | 6.93 |
| CHEMBL541736 | — | — | 1 | 6.92 |
| CHEMBL560711 | — | — | 1 | 6.91 |
| CHEMBL539653 | — | — | 1 | 6.86 |
| CHEMBL555436 | — | — | 1 | 6.83 |
| CHEMBL557343 | — | — | 1 | 6.79 |
| CHEMBL556626 | — | — | 1 | 6.79 |
| CHEMBL550643 | — | — | 1 | 6.74 |
| CHEMBL541739 | — | — | 1 | 6.74 |
| CHEMBL541170 | — | — | 1 | 6.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539973 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL538636 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL540729 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL553571 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL552743 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL555517 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL539466 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL553612 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL539465 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL538637 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL221597 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL551980 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL563604 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL558938 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL539975 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL555916 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL553458 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL553457 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL541976 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL557554 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL557352 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL541736 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL560711 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL539653 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL555436 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL557343 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL556626 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL550643 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL541739 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL541170 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL558946 | — | IC50 | = | 205.0 | nM | 6.69 |
| CHEMBL558894 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL555519 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL555435 | — | IC50 | = | 266.0 | nM | 6.58 |
| CHEMBL539467 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL541977 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL541020 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL552323 | — | IC50 | = | 363.0 | nM | 6.44 |
| CHEMBL540730 | — | IC50 | = | 367.0 | nM | 6.43 |
| CHEMBL558542 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL539654 | — | IC50 | = | 412.0 | nM | 6.38 |
| CHEMBL540731 | — | IC50 | = | 429.0 | nM | 6.37 |
| CHEMBL553424 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL555518 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL539972 | — | IC50 | = | 534.0 | nM | 6.27 |
| CHEMBL550753 | — | IC50 | = | 559.0 | nM | 6.25 |
| CHEMBL553456 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL541738 | — | IC50 | = | 821.0 | nM | 6.09 |
| CHEMBL552744 | — | IC50 | = | 1232.0 | nM | 5.91 |
| CHEMBL555520 | — | IC50 | = | 2098.0 | nM | 5.68 |