Assay Detail
Binding
CHEMBL1177263
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Modulation of gamma-secretase-mediated cleavage of human APP expressed in CHO cells with human presenilin-1 assessed as inhibition of amyloid beta42 production after 24 hrs by ELISA
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis, and biological evaluation of a novel class of gamma-secretase modulators with PPARgamma activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 4.69 | 5.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171834 | — | — | 1 | 5.29 |
| CHEMBL1170264 | — | — | 1 | 5.22 |
| CHEMBL1170852 | — | — | 1 | 5.07 |
| CHEMBL1171833 | — | — | 1 | 4.95 |
| CHEMBL1173376 | — | — | 1 | 4.89 |
| CHEMBL1172000 | — | — | 1 | 4.76 |
| CHEMBL1173121 | — | — | 1 | 4.71 |
| CHEMBL1173564 | — | — | 1 | 4.67 |
| CHEMBL461883 | — | — | 1 | 4.64 |
| CHEMBL1172016 | — | — | 1 | 4.64 |
| CHEMBL1172222 | — | — | 1 | 4.60 |
| CHEMBL6 | INDOMETHACIN | 4.0 | 1 | 4.60 |
| CHEMBL1172002 | — | — | 1 | 4.55 |
| CHEMBL1171851 | — | — | 1 | 4.53 |
| CHEMBL1172003 | — | — | 1 | 4.52 |
| CHEMBL1172019 | — | — | 1 | 4.51 |
| CHEMBL1171652 | — | — | 1 | 4.51 |
| CHEMBL1170076 | — | — | 1 | 4.49 |
| CHEMBL18797 | SULINDAC SULFIDE | -1.0 | 1 | 4.47 |
| CHEMBL1171832 | — | — | 1 | 4.42 |
| CHEMBL1173499 | — | — | 1 | 4.38 |
| CHEMBL521 | IBUPROFEN | 4.0 | 1 | - |
| CHEMBL1171831 | — | — | 1 | - |
| CHEMBL518507 | — | — | 1 | - |
| CHEMBL1316 | CARPROFEN | 4.0 | 1 | - |
| CHEMBL1172001 | — | — | 1 | - |
| CHEMBL190083 | TARENFLURBIL | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171834 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL1170264 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1170852 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL1171833 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL1173376 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1172000 | — | IC50 | = | 17200.0 | nM | 4.76 |
| CHEMBL1173121 | — | IC50 | = | 19300.0 | nM | 4.71 |
| CHEMBL1173564 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL461883 | — | IC50 | = | 22800.0 | nM | 4.64 |
| CHEMBL1172016 | — | IC50 | = | 22900.0 | nM | 4.64 |
| CHEMBL1172222 | — | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL6 | INDOMETHACIN | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL1172002 | — | IC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL1171851 | — | IC50 | = | 29300.0 | nM | 4.53 |
| CHEMBL1172003 | — | IC50 | = | 30400.0 | nM | 4.52 |
| CHEMBL1172019 | — | IC50 | = | 30900.0 | nM | 4.51 |
| CHEMBL1171652 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL1170076 | — | IC50 | = | 32600.0 | nM | 4.49 |
| CHEMBL18797 | SULINDAC SULFIDE | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL1171832 | — | IC50 | = | 37700.0 | nM | 4.42 |
| CHEMBL1173499 | — | IC50 | = | 41600.0 | nM | 4.38 |
| CHEMBL521 | IBUPROFEN | IC50 | = | 200000.0 | nM | - |
| CHEMBL1171831 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL518507 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1316 | CARPROFEN | IC50 | = | 305000.0 | nM | - |
| CHEMBL1172001 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL190083 | TARENFLURBIL | IC50 | = | 305000.0 | nM | - |