Assay Detail
Binding
CHEMBL5049075
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Inhibition of human GCS using C8-ceramide and UDP-glucose as substrate incubated for 1 hr by RapidFire mass spectrometry
26
Total Activities
26
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 Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.47 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085509 | — | — | 1 | 7.82 |
| CHEMBL5092141 | — | — | 1 | 7.77 |
| CHEMBL5083428 | — | — | 1 | 7.72 |
| CHEMBL5078078 | — | — | 1 | 7.51 |
| CHEMBL5077442 | — | — | 1 | 7.40 |
| CHEMBL5086168 | — | — | 1 | 7.35 |
| CHEMBL5086523 | — | — | 1 | 7.31 |
| CHEMBL5091974 | — | — | 1 | 7.31 |
| CHEMBL5076612 | — | — | 1 | 7.01 |
| CHEMBL5091003 | — | — | 1 | 6.77 |
| CHEMBL5089984 | — | — | 1 | 6.20 |
| CHEMBL5081829 | — | — | 1 | 6.16 |
| CHEMBL5088946 | — | — | 1 | 6.00 |
| CHEMBL5083924 | — | — | 1 | 5.89 |
| CHEMBL5090560 | — | — | 1 | 5.72 |
| CHEMBL5074066 | — | — | 1 | 5.62 |
| CHEMBL5069925 | — | — | 1 | 5.50 |
| CHEMBL5085654 | — | — | 1 | 5.36 |
| CHEMBL5071935 | — | — | 1 | 5.36 |
| CHEMBL5081824 | — | — | 1 | 5.31 |
| CHEMBL5093384 | — | — | 1 | 4.77 |
| CHEMBL5069574 | — | — | 1 | - |
| CHEMBL5085627 | — | — | 1 | - |
| CHEMBL5085407 | — | — | 1 | - |
| CHEMBL5082608 | — | — | 1 | - |
| CHEMBL5083606 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085509 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5092141 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5083428 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5078078 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5077442 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5086168 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5086523 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5091974 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5076612 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5091003 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5089984 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5081829 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5088946 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5083924 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5090560 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5074066 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL5069925 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5085654 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5071935 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5081824 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5093384 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5069574 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5085627 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5085407 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5082608 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5083606 | — | IC50 | > | 100000.0 | nM | - |