Assay Detail
Binding
CHEMBL2183602
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Inhibition of human ACAT1 by liquid scintillography
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.61 | 5.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178947 | — | — | 1 | 5.62 |
| CHEMBL2178371 | — | — | 1 | 4.82 |
| CHEMBL2178384 | — | — | 1 | 4.80 |
| CHEMBL2178935 | — | — | 1 | 4.60 |
| CHEMBL4297354 | AZD-7687 | 1.0 | 1 | 4.47 |
| CHEMBL2178940 | — | — | 1 | 4.36 |
| CHEMBL2178933 | — | — | 1 | 4.12 |
| CHEMBL2178950 | — | — | 1 | 4.10 |
| CHEMBL2178939 | — | — | 1 | - |
| CHEMBL2178938 | — | — | 1 | - |
| CHEMBL2178937 | — | — | 1 | - |
| CHEMBL2178936 | — | — | 1 | - |
| CHEMBL2178934 | — | — | 1 | - |
| CHEMBL2178952 | — | — | 1 | - |
| CHEMBL2178951 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178947 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2178371 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2178384 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL2178935 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL4297354 | AZD-7687 | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL2178940 | — | IC50 | = | 44000.0 | nM | 4.36 |
| CHEMBL2178933 | — | IC50 | = | 75000.0 | nM | 4.12 |
| CHEMBL2178950 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL2178939 | — | IC50 | - | — | - | |
| CHEMBL2178938 | — | IC50 | - | — | - | |
| CHEMBL2178937 | — | IC50 | - | — | - | |
| CHEMBL2178936 | — | IC50 | - | — | - | |
| CHEMBL2178934 | — | IC50 | - | — | - | |
| CHEMBL2178952 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2178951 | — | IC50 | > | 33000.0 | nM | - |