Assay Detail
Binding
CHEMBL4836595
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Inhibition of MTase activity of N-terminal 6XHis-tagged SARS-CoV-2 NSP14 expressed in Escherichia coli BL21(DE3) using GpppG and SAM as substrate incubated for 20 mins 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 | 6.12 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874278 | — | — | 1 | 8.10 |
| CHEMBL4850353 | — | — | 1 | 6.80 |
| CHEMBL4875728 | — | — | 1 | 6.52 |
| CHEMBL1214186 | SINEFUNGIN | 2.0 | 1 | 6.35 |
| CHEMBL4869943 | — | — | 1 | 6.18 |
| CHEMBL4849284 | — | — | 1 | 6.16 |
| CHEMBL4870702 | — | — | 1 | 5.19 |
| CHEMBL4857500 | — | — | 1 | 4.92 |
| CHEMBL4868791 | — | — | 1 | 4.90 |
| CHEMBL4872017 | — | — | 1 | - |
| CHEMBL4872937 | — | — | 1 | - |
| CHEMBL4851408 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874278 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4850353 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4875728 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1214186 | SINEFUNGIN | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4869943 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4849284 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL4870702 | — | IC50 | = | 6480.0 | nM | 5.19 |
| CHEMBL4857500 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4868791 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL4872017 | — | IC50 | = | 233000.0 | nM | - |
| CHEMBL4872937 | — | IC50 | - | — | - | |
| CHEMBL4851408 | — | IC50 | = | 215000.0 | nM | - |