Assay Detail
Binding
CHEMBL3136463
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Inhibition of recombinant human DGAT1 expressed in sf9 cell membrane assessed as inhibition of radioactive trioleoylglycerol formation after 30 mins by liquid scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 the discovery of AZD2353
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.89 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3133098 | — | — | 1 | 8.20 |
| CHEMBL3133093 | — | — | 1 | 8.10 |
| CHEMBL3133091 | — | — | 1 | 8.10 |
| CHEMBL3133092 | — | — | 1 | 7.90 |
| CHEMBL3133087 | — | — | 1 | 7.70 |
| CHEMBL3133088 | — | — | 1 | 7.60 |
| CHEMBL3133094 | — | — | 1 | 7.00 |
| CHEMBL3133095 | — | — | 1 | 6.90 |
| CHEMBL3133096 | — | — | 1 | 6.90 |
| CHEMBL3133089 | — | — | 1 | 6.70 |
| CHEMBL3133086 | — | — | 1 | 6.50 |
| CHEMBL3133100 | — | — | 1 | 6.20 |
| CHEMBL3133090 | — | — | 1 | 6.10 |
| CHEMBL3133097 | — | — | 1 | 5.90 |
| CHEMBL3133085 | — | — | 1 | 5.20 |
| CHEMBL3133099 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3133098 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL3133093 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3133091 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL3133092 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL3133087 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL3133088 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3133094 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3133095 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3133096 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL3133089 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL3133086 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3133100 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3133090 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3133097 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3133085 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3133099 | — | IC50 | = | 6309.57 | nM | 5.20 |