Assay Detail
Binding
CHEMBL5578428
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal his-tagged SARS CoV-2 PL protease (1564 to 1878 residues) expressed in BL21 (DE3) cells using Z-RLRGG-AMC as substrate preincubated for 10 mins followed by substrate addition and measured for 15 mins by fluorescence based analysis
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Severe acute respiratory syndrome coronavirus 2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Replicase polyprotein 1ab (CHEMBL4523582) ↗| Type | SINGLE PROTEIN |
| Organism | Severe acute respiratory syndrome coronavirus 2 |
Publication
Non-Covalent Inhibitors of SARS-CoV-2 Papain-Like Protease (PLpro): In Vitro and In Vivo Antiviral Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 57 | 6.02 | 6.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5079592 | — | — | 1 | 6.95 |
| CHEMBL5085054 | — | — | 1 | 6.68 |
| CHEMBL5591637 | — | — | 1 | 6.58 |
| CHEMBL5590755 | — | — | 1 | 6.50 |
| CHEMBL5183892 | — | — | 1 | 6.48 |
| CHEMBL5594376 | — | — | 1 | 6.48 |
| CHEMBL5583676 | — | — | 1 | 6.44 |
| CHEMBL5085659 | — | — | 1 | 6.43 |
| CHEMBL5591371 | — | — | 1 | 6.42 |
| CHEMBL5078524 | — | — | 1 | 6.41 |
| CHEMBL5591153 | — | — | 1 | 6.37 |
| CHEMBL5583933 | — | — | 1 | 6.33 |
| CHEMBL5591613 | — | — | 1 | 6.31 |
| CHEMBL5594740 | — | — | 1 | 6.30 |
| CHEMBL5592166 | — | — | 1 | 6.26 |
| CHEMBL5593811 | — | — | 1 | 6.25 |
| CHEMBL5083635 | — | — | 1 | 6.25 |
| CHEMBL5595950 | — | — | 1 | 6.24 |
| CHEMBL5591278 | — | — | 1 | 6.22 |
| CHEMBL5592606 | — | — | 1 | 6.22 |
| CHEMBL5594403 | — | — | 1 | 6.21 |
| CHEMBL5583811 | — | — | 1 | 6.19 |
| CHEMBL5591703 | — | — | 1 | 6.16 |
| CHEMBL5590148 | — | — | 1 | 6.12 |
| CHEMBL5594581 | — | — | 1 | 6.10 |
| CHEMBL5591014 | — | — | 1 | 6.09 |
| CHEMBL5592435 | — | — | 1 | 6.09 |
| CHEMBL5593630 | — | — | 1 | 6.09 |
| CHEMBL5584015 | — | — | 1 | 6.04 |
| CHEMBL5589924 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5079592 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL5085054 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5591637 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5590755 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5183892 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5594376 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5583676 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5085659 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5591371 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5078524 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5591153 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5583933 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5591613 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5594740 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5592166 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5593811 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5083635 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5595950 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5591278 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5592606 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL5594403 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5583811 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5591703 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL5590148 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5594581 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5591014 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5593630 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL5592435 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5584015 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5589924 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL5589927 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL5590536 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL5589705 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL5592351 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL5589680 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL5591155 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5583810 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL5594045 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL5592713 | — | IC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5088866 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL5595528 | — | IC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL5592033 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL549695 | — | IC50 | = | 1610.0 | nM | 5.79 |
| CHEMBL5591998 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL5594115 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL5595314 | — | IC50 | = | 1790.0 | nM | 5.75 |
| CHEMBL5590671 | — | IC50 | = | 1960.0 | nM | 5.71 |
| CHEMBL5593629 | — | IC50 | = | 1930.0 | nM | 5.71 |
| CHEMBL5590827 | — | IC50 | = | 2420.0 | nM | 5.62 |
| CHEMBL5594527 | — | IC50 | = | 2400.0 | nM | 5.62 |