Assay Detail
Binding
CHEMBL1107112
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Inhibition of gamma-secretase-mediated notch cleavage in human SNC cells by ELISA
22
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SNC |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.48 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089001 | ENT A | — | 2 | 7.16 |
| CHEMBL1093761 | — | — | 1 | 6.53 |
| CHEMBL1090408 | — | — | 1 | 6.13 |
| CHEMBL1088999 | — | — | 1 | 5.80 |
| CHEMBL1092102 | — | — | 1 | 5.64 |
| CHEMBL1093400 | — | — | 1 | 5.59 |
| CHEMBL1093401 | — | — | 1 | 5.27 |
| CHEMBL1093399 | — | — | 1 | 5.19 |
| CHEMBL1092488 | — | — | 1 | 5.18 |
| CHEMBL1092100 | — | — | 1 | 5.17 |
| CHEMBL2447970 | — | — | 1 | 5.16 |
| CHEMBL1092141 | — | — | 1 | 4.99 |
| CHEMBL1093402 | — | — | 1 | 4.94 |
| CHEMBL1093403 | — | — | 1 | 4.85 |
| CHEMBL1089000 | — | — | 1 | 4.81 |
| CHEMBL1089961 | — | — | 1 | 4.78 |
| CHEMBL1092487 | — | — | 1 | 4.47 |
| CHEMBL1092101 | — | — | 1 | - |
| CHEMBL1092452 | — | — | 1 | - |
| CHEMBL1090406 | — | — | 1 | - |
| CHEMBL1090407 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089001 | ENT A | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL1089001 | ENT A | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL1093761 | — | IC50 | = | 295.0 | nM | 6.53 |
| CHEMBL1090408 | — | IC50 | = | 736.0 | nM | 6.13 |
| CHEMBL1088999 | — | IC50 | = | 1568.0 | nM | 5.80 |
| CHEMBL1092102 | — | IC50 | = | 2305.0 | nM | 5.64 |
| CHEMBL1093400 | — | IC50 | = | 2586.0 | nM | 5.59 |
| CHEMBL1093401 | — | IC50 | = | 5319.0 | nM | 5.27 |
| CHEMBL1093399 | — | IC50 | = | 6514.0 | nM | 5.19 |
| CHEMBL1092488 | — | IC50 | = | 6527.0 | nM | 5.18 |
| CHEMBL1092100 | — | IC50 | = | 6759.0 | nM | 5.17 |
| CHEMBL2447970 | — | IC50 | = | 6854.0 | nM | 5.16 |
| CHEMBL1092141 | — | IC50 | = | 10263.0 | nM | 4.99 |
| CHEMBL1093402 | — | IC50 | = | 11397.0 | nM | 4.94 |
| CHEMBL1093403 | — | IC50 | = | 14126.0 | nM | 4.85 |
| CHEMBL1089000 | — | IC50 | = | 15455.0 | nM | 4.81 |
| CHEMBL1089961 | — | IC50 | = | 16625.0 | nM | 4.78 |
| CHEMBL1092487 | — | IC50 | = | 33565.0 | nM | 4.47 |
| CHEMBL1092101 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1092452 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1090406 | — | IC50 | > | 40000.0 | nM | - |
| CHEMBL1090407 | — | IC50 | > | 40000.0 | nM | - |