Assay Detail
Binding
CHEMBL4480313
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Inhibition of ATG4B (unknown origin) using His-GATE-16-GST as substrate preincubated for 30 mins followed by substrate addition measured after 30 mins by TR-FRET assay
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 5.72 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4581663 | — | — | 1 | 7.24 |
| CHEMBL4520267 | — | — | 1 | 7.10 |
| CHEMBL4546760 | — | — | 1 | 6.96 |
| CHEMBL4553669 | — | — | 1 | 6.72 |
| CHEMBL4520585 | — | — | 1 | 6.68 |
| CHEMBL4567870 | — | — | 1 | 6.57 |
| CHEMBL4578571 | — | — | 1 | 6.14 |
| CHEMBL4588146 | — | — | 1 | 6.00 |
| CHEMBL4579064 | — | — | 1 | 6.00 |
| CHEMBL4535723 | — | — | 1 | 5.98 |
| CHEMBL4567655 | — | — | 1 | 5.97 |
| CHEMBL4539211 | — | — | 1 | 5.96 |
| CHEMBL4572200 | — | — | 1 | 5.95 |
| CHEMBL4590201 | — | — | 1 | 5.92 |
| CHEMBL4569375 | — | — | 1 | 5.73 |
| CHEMBL4562540 | — | — | 1 | 5.70 |
| CHEMBL4554009 | — | — | 1 | 5.44 |
| CHEMBL4574173 | — | — | 1 | 5.42 |
| CHEMBL4570064 | — | — | 1 | 5.38 |
| CHEMBL4566679 | — | — | 1 | 5.32 |
| CHEMBL4525169 | — | — | 1 | 5.19 |
| CHEMBL4527514 | — | — | 1 | 5.04 |
| CHEMBL4540188 | — | — | 1 | 4.93 |
| CHEMBL2402203 | — | — | 1 | 4.82 |
| CHEMBL4556657 | — | — | 1 | 4.75 |
| CHEMBL4566110 | — | — | 1 | 4.49 |
| CHEMBL4515617 | — | — | 1 | 4.48 |
| CHEMBL4564704 | — | — | 1 | 4.26 |
| CHEMBL4520698 | — | — | 1 | - |
| CHEMBL4529816 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4581663 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4520267 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4546760 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4553669 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4520585 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4567870 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4578571 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4588146 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4579064 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4535723 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL4567655 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4539211 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4572200 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL4590201 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4569375 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4562540 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4554009 | — | IC50 | = | 3610.0 | nM | 5.44 |
| CHEMBL4574173 | — | IC50 | = | 3760.0 | nM | 5.42 |
| CHEMBL4570064 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL4566679 | — | IC50 | = | 4790.0 | nM | 5.32 |
| CHEMBL4525169 | — | IC50 | = | 6480.0 | nM | 5.19 |
| CHEMBL4527514 | — | IC50 | = | 9130.0 | nM | 5.04 |
| CHEMBL4540188 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL2402203 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL4556657 | — | IC50 | = | 17800.0 | nM | 4.75 |
| CHEMBL4566110 | — | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL4515617 | — | IC50 | = | 33100.0 | nM | 4.48 |
| CHEMBL4564704 | — | IC50 | = | 55100.0 | nM | 4.26 |
| CHEMBL4568708 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4594129 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4527093 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4555270 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4218185 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4549686 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL344174 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4204523 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4563886 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4529816 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL4520698 | — | IC50 | > | 200000.0 | nM | - |