Assay Detail
Binding
CHEMBL4845052
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of rat recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase (CHEMBL4879456) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.19 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3893594 | — | — | 1 | 8.51 |
| CHEMBL4878564 | — | — | 1 | 8.07 |
| CHEMBL3912712 | BMS-963272 | 1.0 | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3893594 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4878564 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL3912712 | BMS-963272 | IC50 | = | 10.0 | nM | 8.00 |