Assay Detail
Binding
CHEMBL3887138
Review assay metadata, readout intent, target linkage, and publication context from the same page.
MGAT SPA Assay: MGAT2 enzyme was assayed using membranes isolated from Sf9 cells expressing the recombinant human MGAT2 cDNA with 2-monooleoylglycerol and [3H]-oleoyl-CoA as substrates as described by Seethala et al. [Anal. Biochem., 383(2):144-150 (Dec. 15, 2008)]. Briefly, the assays were conducted in 384-well plates in a total volume of 30 uL at 25° C. In each assay, 200 ng of recombinant human MGAT2 membrane was incubated with 10 uM of 2-monooleoylglycerol and 15 uM of [3H]-oleoyl-CoA in 100 mM potassium phosphate (pH 7.4) for 20 min with various concentrations of compounds delivered in DMSO. The assay was terminated by the addition of 20 ul of Stopping Solution (7.5 mg/ml Yttrium Oxide Polylysine beads, 3.3 mg/ml Fraction V BSA and 200 uM Mercuric chloride in 50 mM HEPES, pH 7.4). The signal was measured 1 h after quenching the reaction using LEADSEEKERSM for 5 minutes. To calculate the degree of inhibition, the zero level of enzyme activity (blank) was defined.
142
Total Activities
127
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Liver |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase (CHEMBL2321630) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aryl dihydropyridinones and piperidinone MGAT2 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 142 | 6.40 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3934758 | — | — | 1 | 8.10 |
| CHEMBL3929176 | — | — | 1 | 8.05 |
| CHEMBL3932589 | — | — | 1 | 7.96 |
| CHEMBL3963796 | — | — | 1 | 7.96 |
| CHEMBL3893594 | — | — | 1 | 7.85 |
| CHEMBL3981198 | — | — | 1 | 7.85 |
| CHEMBL2441600 | — | — | 2 | 7.82 |
| CHEMBL3925829 | — | — | 1 | 7.80 |
| CHEMBL3937187 | — | — | 1 | 7.70 |
| CHEMBL3973375 | — | — | 1 | 7.68 |
| CHEMBL3906382 | — | — | 1 | 7.66 |
| CHEMBL3954459 | — | — | 1 | 7.62 |
| CHEMBL3917264 | — | — | 1 | 7.60 |
| CHEMBL3967083 | — | — | 1 | 7.55 |
| CHEMBL3897522 | — | — | 1 | 7.50 |
| CHEMBL3986742 | — | — | 1 | 7.50 |
| CHEMBL3930463 | — | — | 1 | 7.47 |
| CHEMBL3966030 | — | — | 2 | 7.46 |
| CHEMBL3970593 | — | — | 1 | 7.44 |
| CHEMBL3911717 | — | — | 1 | 7.43 |
| CHEMBL3897024 | — | — | 1 | 7.37 |
| CHEMBL3979985 | — | — | 1 | 7.33 |
| CHEMBL3895659 | — | — | 1 | 7.32 |
| CHEMBL3977050 | — | — | 1 | 7.32 |
| CHEMBL3902676 | — | — | 1 | 7.28 |
| CHEMBL3957613 | — | — | 1 | 7.28 |
| CHEMBL3973007 | — | — | 2 | 7.26 |
| CHEMBL3892111 | — | — | 1 | 7.24 |
| CHEMBL3978458 | — | — | 2 | 7.22 |
| CHEMBL3916973 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3934758 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3929176 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3932589 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3963796 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3893594 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3981198 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2441600 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3925829 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3937187 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3973375 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3906382 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3954459 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3917264 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3967083 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3986742 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3897522 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3930463 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3966030 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3970593 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3911717 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3897024 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL3979985 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3895659 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3977050 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3957613 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3902676 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3973007 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3892111 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3978458 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3916973 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3966030 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3963586 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3961967 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL3931860 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3900943 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL3894666 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3963586 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3956480 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3890409 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL3919277 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL3931860 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3950677 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3907985 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL3943482 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3972008 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL3955595 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL3955945 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3973558 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL3898522 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL3902329 | — | IC50 | = | 158.0 | nM | 6.80 |