Assay Detail
Binding
CHEMBL4836596
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Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 Wuhan-Hu-1 NSP16/10 expressed in Escherichia coli using m7GpppA-RNA and SAM as substrate incubated for 2 hrs by HTRF assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Severe acute respiratory syndrome coronavirus 2 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Potent SARS-CoV-2 mRNA Cap Methyltransferase Inhibitors by Bioisosteric Replacement of Methionine in SAM Cosubstrate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.36 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874278 | — | — | 1 | 8.40 |
| CHEMBL4850353 | — | — | 1 | 7.40 |
| CHEMBL4875728 | — | — | 1 | 7.00 |
| CHEMBL4869943 | — | — | 1 | 6.33 |
| CHEMBL1214186 | SINEFUNGIN | 2.0 | 1 | 6.07 |
| CHEMBL4849284 | — | — | 1 | 6.04 |
| CHEMBL4857500 | — | — | 1 | 5.80 |
| CHEMBL4870702 | — | — | 1 | 5.40 |
| CHEMBL4868791 | — | — | 1 | 4.82 |
| CHEMBL4872017 | — | — | 1 | - |
| CHEMBL4872937 | — | — | 1 | - |
| CHEMBL4851408 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874278 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4850353 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4875728 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4869943 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL1214186 | SINEFUNGIN | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4849284 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL4857500 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL4870702 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4868791 | — | IC50 | = | 15300.0 | nM | 4.82 |
| CHEMBL4872017 | — | IC50 | = | 121000.0 | nM | - |
| CHEMBL4872937 | — | IC50 | - | — | - | |
| CHEMBL4851408 | — | IC50 | = | 223000.0 | nM | - |