Assay Detail
Functional
CHEMBL833176
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In vitro inhibitory concentration against human Microsomal triglyceride transfer protein
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Microsomal triglyceride transfer protein large subunit (CHEMBL2569) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 7.99 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL186836 | — | — | 1 | 8.52 |
| CHEMBL184354 | — | — | 1 | 8.30 |
| CHEMBL365687 | — | — | 2 | 8.15 |
| CHEMBL354541 | LOMITAPIDE | 4.0 | 1 | 8.10 |
| CHEMBL360146 | — | — | 1 | 8.05 |
| CHEMBL186494 | — | — | 1 | 8.05 |
| CHEMBL185866 | — | — | 1 | 7.96 |
| CHEMBL187076 | — | — | 1 | 7.92 |
| CHEMBL187696 | — | — | 1 | 7.85 |
| CHEMBL282785 | — | — | 1 | 7.66 |
| CHEMBL184221 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL186836 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL184354 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL365687 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL354541 | LOMITAPIDE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL360146 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL186494 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL185866 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL187076 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL187696 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL282785 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL365687 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL184221 | — | IC50 | < | 10.0 | nM | - |