Assay Detail
Binding
CHEMBL2343709
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Inhibition of human DGAT1 expressed in Sf9 cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-Co A substrates incubated for 2 hrs by scintillation counting method
35
Total Activities
35
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
Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.97 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2334097 | — | — | 1 | 7.62 |
| CHEMBL2334088 | — | — | 1 | 7.60 |
| CHEMBL2334082 | — | — | 1 | 7.54 |
| CHEMBL2334075 | — | — | 1 | 7.48 |
| CHEMBL1766813 | — | — | 1 | 7.42 |
| CHEMBL2334093 | — | — | 1 | 7.41 |
| CHEMBL2334092 | — | — | 1 | 7.40 |
| CHEMBL2334085 | — | — | 1 | 7.39 |
| CHEMBL2334095 | — | — | 1 | 7.38 |
| CHEMBL2334094 | — | — | 1 | 7.29 |
| CHEMBL2334100 | — | — | 1 | 7.28 |
| CHEMBL2334081 | — | — | 1 | 7.27 |
| CHEMBL2334089 | — | — | 1 | 7.26 |
| CHEMBL2334091 | — | — | 1 | 7.22 |
| CHEMBL2334098 | — | — | 1 | 7.16 |
| CHEMBL2334078 | — | — | 1 | 7.10 |
| CHEMBL2334096 | — | — | 1 | 6.99 |
| CHEMBL2334079 | — | — | 1 | 6.94 |
| CHEMBL2334070 | — | — | 1 | 6.92 |
| CHEMBL2334071 | — | — | 1 | 6.92 |
| CHEMBL2334068 | — | — | 1 | 6.90 |
| CHEMBL2334090 | — | — | 1 | 6.84 |
| CHEMBL2334084 | — | — | 1 | 6.83 |
| CHEMBL2334069 | — | — | 1 | 6.82 |
| CHEMBL2334087 | — | — | 1 | 6.72 |
| CHEMBL2334077 | — | — | 1 | 6.71 |
| CHEMBL2334072 | — | — | 1 | 6.62 |
| CHEMBL2334101 | — | — | 1 | 6.55 |
| CHEMBL2334099 | — | — | 1 | 6.51 |
| CHEMBL2334076 | — | — | 1 | 6.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2334097 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2334088 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2334082 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2334075 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL1766813 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2334093 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2334092 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2334085 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2334095 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL2334094 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2334100 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2334081 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2334089 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL2334091 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2334098 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2334078 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2334096 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL2334079 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL2334071 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2334070 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL2334068 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL2334090 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL2334084 | — | IC50 | = | 149.0 | nM | 6.83 |
| CHEMBL2334069 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL2334087 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2334077 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL2334072 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2334101 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2334099 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL2334076 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL2334083 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL2334080 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL2334074 | — | IC50 | = | 482.0 | nM | 6.32 |
| CHEMBL2334086 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL2334073 | — | IC50 | = | 774.0 | nM | 6.11 |