Assay Detail
Binding
CHEMBL5734977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzymatic Activity Assay: DGAT2 activity was determined by measuring the amount of enzymatic product triolein (1,2,3-Tri(cis-9-octadecenoyl)glycerol) using the membrane prep mentioned above. The assay was carried out in deep well 384 plates in a final volume of 40 μL at room temperature. The assay mixture contained the following: assay buffer (100 mM Tris.Cl, pH 7.0, 20 mM MgCl2, 5% ethanol), 25 μM of diolein, 10 μM of oleoyl-CoA and 10 ng/μL of DGAT2 membrane.
423
Total Activities
138
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 141 | 6.49 | 9.18 |
| kon | 141 | - | - |
| k_off | 141 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6000290 | — | — | 3 | 9.18 |
| CHEMBL5991270 | — | — | 3 | 8.95 |
| CHEMBL6060795 | — | — | 3 | 8.66 |
| CHEMBL5849208 | — | — | 3 | 8.52 |
| CHEMBL5938206 | — | — | 3 | 8.44 |
| CHEMBL5775051 | — | — | 3 | 8.44 |
| CHEMBL5942569 | — | — | 3 | 8.24 |
| CHEMBL5938338 | — | — | 3 | 8.24 |
| CHEMBL5753425 | — | — | 3 | 8.21 |
| CHEMBL5860266 | — | — | 3 | 8.08 |
| CHEMBL5882372 | — | — | 3 | 8.07 |
| CHEMBL6040965 | — | — | 3 | 8.03 |
| CHEMBL5985921 | — | — | 3 | 8.01 |
| CHEMBL5755785 | — | — | 3 | 8.00 |
| CHEMBL5954660 | — | — | 3 | 7.98 |
| CHEMBL5802239 | — | — | 3 | 7.94 |
| CHEMBL6058144 | — | — | 3 | 7.94 |
| CHEMBL5965391 | — | — | 3 | 7.94 |
| CHEMBL6013100 | — | — | 3 | 7.93 |
| CHEMBL5891481 | — | — | 3 | 7.87 |
| CHEMBL5910959 | — | — | 3 | 7.87 |
| CHEMBL5802038 | — | — | 3 | 7.86 |
| CHEMBL6041971 | — | — | 6 | 7.81 |
| CHEMBL5908278 | — | — | 3 | 7.79 |
| CHEMBL6011379 | — | — | 3 | 7.71 |
| CHEMBL5805848 | — | — | 3 | 7.70 |
| CHEMBL6052343 | — | — | 3 | 7.69 |
| CHEMBL5770881 | — | — | 3 | 7.65 |
| CHEMBL5841950 | — | — | 3 | 7.62 |
| CHEMBL6063237 | — | — | 3 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6000290 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL5991270 | — | IC50 | = | 1.13 | nM | 8.95 |
| CHEMBL6060795 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5849208 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5938206 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5775051 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5942569 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5938338 | — | IC50 | = | 5.78 | nM | 8.24 |
| CHEMBL5753425 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5860266 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5882372 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL6040965 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5985921 | — | IC50 | = | 9.88 | nM | 8.01 |
| CHEMBL5755785 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5954660 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL6058144 | — | IC50 | = | 11.5 | nM | 7.94 |
| CHEMBL5802239 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL5965391 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL6013100 | — | IC50 | = | 11.7 | nM | 7.93 |
| CHEMBL5910959 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL5891481 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL5802038 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL6041971 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL6041971 | — | IC50 | = | 15.5 | nM | 7.81 |
| CHEMBL5908278 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL6011379 | — | IC50 | = | 19.6 | nM | 7.71 |
| CHEMBL5805848 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL6052343 | — | IC50 | = | 20.4 | nM | 7.69 |
| CHEMBL5770881 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5841950 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL6063237 | — | IC50 | = | 23.8 | nM | 7.62 |
| CHEMBL6001413 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5773264 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5841307 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5745828 | — | IC50 | = | 59.8 | nM | 7.22 |
| CHEMBL5913214 | — | IC50 | = | 82.3 | nM | 7.08 |
| CHEMBL5751746 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5942728 | — | IC50 | = | 89.8 | nM | 7.05 |
| CHEMBL6011523 | — | IC50 | = | 95.6 | nM | 7.02 |
| CHEMBL5919685 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5837225 | — | IC50 | = | 97.6 | nM | 7.01 |
| CHEMBL5915079 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6043343 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL5815118 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5891025 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL6050219 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5891891 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5811365 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5884430 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL6046359 | — | IC50 | = | 209.0 | nM | 6.68 |