Assay Detail
Binding
CHEMBL5237300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length N-terminal his6-tagged human CH24H (28 to 494 residues) expressed in Escherichia coli DH5alpha using [14C] cholesterol as substrate preincubated for 15 mins followed by substrate addition and measured after 5 min in presence of beta-NADPH
30
Total Activities
30
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
Discovery of Soticlestat, a Potent and Selective Inhibitor for Cholesterol 24-Hydroxylase (CH24H).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.47 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5279173 | — | — | 1 | 9.00 |
| CHEMBL5288661 | — | — | 1 | 8.62 |
| CHEMBL5276973 | — | — | 1 | 8.57 |
| CHEMBL5282804 | — | — | 1 | 8.37 |
| CHEMBL5271033 | — | — | 1 | 8.36 |
| CHEMBL5269674 | — | — | 1 | 8.33 |
| CHEMBL5289771 | — | — | 1 | 8.31 |
| CHEMBL5284673 | — | — | 1 | 8.21 |
| CHEMBL4298172 | SOTICLESTAT | 3.0 | 1 | 8.13 |
| CHEMBL5275089 | — | — | 1 | 8.11 |
| CHEMBL5275183 | — | — | 1 | 8.10 |
| CHEMBL5286208 | — | — | 1 | 7.80 |
| CHEMBL5274224 | — | — | 1 | 7.77 |
| CHEMBL5269081 | — | — | 1 | 7.68 |
| CHEMBL5272679 | — | — | 1 | 7.44 |
| CHEMBL5285548 | — | — | 1 | 7.22 |
| CHEMBL5282243 | — | — | 1 | 7.13 |
| CHEMBL5267408 | — | — | 1 | 7.05 |
| CHEMBL5288871 | — | — | 1 | 7.03 |
| CHEMBL5269664 | — | — | 1 | 7.00 |
| CHEMBL5288993 | — | — | 1 | 6.96 |
| CHEMBL5275961 | — | — | 1 | 6.89 |
| CHEMBL5266978 | — | — | 1 | 6.46 |
| CHEMBL5291094 | — | — | 1 | 6.27 |
| CHEMBL5285292 | — | — | 1 | 5.92 |
| CHEMBL5272278 | — | — | 1 | 5.72 |
| CHEMBL5278891 | — | — | 1 | 5.11 |
| CHEMBL5281369 | — | — | 1 | - |
| CHEMBL5269699 | — | — | 1 | - |
| CHEMBL638 | VORICONAZOLE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5279173 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5288661 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5276973 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5282804 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL5271033 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5269674 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5289771 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5284673 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL4298172 | SOTICLESTAT | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5275089 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5275183 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL5286208 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5274224 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5269081 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5272679 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5285548 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5282243 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5267408 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL5288871 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5269664 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5288993 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5275961 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5266978 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL5291094 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5285292 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5272278 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5278891 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL5281369 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5269699 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL638 | VORICONAZOLE | IC50 | > | 10000.0 | nM | - |