Assay Detail
Binding
CHEMBL1954902
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Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-29 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.68 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1835919 | PF-04620110 | 1.0 | 1 | 8.10 |
| CHEMBL473967 | — | — | 1 | 7.80 |
| CHEMBL1952025 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1835919 | PF-04620110 | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL473967 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1952025 | — | IC50 | = | 71.0 | nM | 7.15 |