Assay Detail
Binding
CHEMBL4845049
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mouse recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCMS assay
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| 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 (CHEMBL2375203) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
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 | 59 | 7.31 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4847167 | — | — | 1 | 8.68 |
| CHEMBL3943482 | — | — | 1 | 8.47 |
| CHEMBL4872250 | — | — | 1 | 8.30 |
| CHEMBL4863471 | — | — | 1 | 8.29 |
| CHEMBL4872517 | — | — | 1 | 8.22 |
| CHEMBL4869563 | — | — | 1 | 8.21 |
| CHEMBL3893594 | — | — | 1 | 8.14 |
| CHEMBL3955595 | — | — | 1 | 8.00 |
| CHEMBL4878564 | — | — | 1 | 7.92 |
| CHEMBL4868038 | — | — | 1 | 7.92 |
| CHEMBL2441600 | — | — | 1 | 7.77 |
| CHEMBL3925202 | — | — | 1 | 7.75 |
| CHEMBL3912712 | BMS-963272 | 1.0 | 1 | 7.75 |
| CHEMBL4875367 | — | — | 1 | 7.75 |
| CHEMBL3963586 | — | — | 1 | 7.70 |
| CHEMBL4872367 | — | — | 1 | 7.66 |
| CHEMBL4862212 | — | — | 1 | 7.64 |
| CHEMBL4873883 | — | — | 1 | 7.55 |
| CHEMBL4865613 | — | — | 1 | 7.50 |
| CHEMBL3902676 | — | — | 1 | 7.43 |
| CHEMBL4848943 | — | — | 1 | 7.42 |
| CHEMBL3963629 | — | — | 1 | 7.42 |
| CHEMBL3985062 | — | — | 1 | 7.34 |
| CHEMBL4864768 | — | — | 1 | 7.32 |
| CHEMBL3984215 | — | — | 1 | 7.29 |
| CHEMBL4854178 | — | — | 1 | 7.26 |
| CHEMBL4878608 | — | — | 1 | 7.26 |
| CHEMBL4865861 | — | — | 1 | 7.23 |
| CHEMBL3911689 | — | — | 1 | 7.18 |
| CHEMBL4869735 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4847167 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3943482 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4872250 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4863471 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4872517 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4869563 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3893594 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL3955595 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4878564 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4868038 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2441600 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3925202 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3912712 | BMS-963272 | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4875367 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3963586 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4872367 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4862212 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4873883 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4865613 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3902676 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4848943 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3963629 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3985062 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4864768 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3984215 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4854178 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4878608 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4865861 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3911689 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4869735 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3919277 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4851952 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3953569 | — | IC50 | = | 118.0 | nM | 6.93 |
| CHEMBL4860076 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4873488 | — | IC50 | = | 164.0 | nM | 6.79 |
| CHEMBL3934122 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3931860 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL3890110 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4863703 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3977988 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4854441 | — | IC50 | = | 315.0 | nM | 6.50 |
| CHEMBL4850770 | — | IC50 | = | 344.0 | nM | 6.46 |
| CHEMBL3961584 | — | IC50 | = | 353.0 | nM | 6.45 |
| CHEMBL4864008 | — | IC50 | = | 448.0 | nM | 6.35 |
| CHEMBL3893559 | — | IC50 | = | 602.0 | nM | 6.22 |
| CHEMBL3964365 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL3916974 | — | IC50 | = | 1052.0 | nM | 5.98 |
| CHEMBL4868511 | — | IC50 | > | 2050.0 | nM | - |
| CHEMBL111 | RIMONABANT | IC50 | - | — | - | |
| CHEMBL4109205 | — | IC50 | > | 2050.0 | nM | - |