Assay Detail
Binding
CHEMBL5736211
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzyme Assay: The total volume of the ATG7 enzymatic assay is 50 μL and contains 50 mM HEPES Hemisodium (pH 7.5), 0.05% BSA, 0.01% Tween-20, 25 mM NaCl, 5 mM MgCl2, 10 μM ATP, 250 μM GSH, 5 nM ATG3-GST, 5 nM Flag-Gabarap, 100 μM TCEP and 0.15 nM recombinant human His-ATG7 enzyme. The enzymatic reaction mixture, with and without inhibitor, was incubated at 24° C. for 105 min in a 384-well plate before termination with 25 μM of Stop/Detection buffer (0.1M HEPES Hemisodium pH 7.5, 0.05% Tween20, 20 mM EDTA, 410 mM KF, 0.53 nM Europium-Cryptate labeled monoclonal anti-Flag M2 Antibody (CisBio International) and 8.125 μg/ml PHYCOLINK goat anti-GST allophycocyanin (XL-APC) antibody (Prozyme)). After incubation for 2 hours at 24° C., quantification of FRET is performed on the Pherostar (BMG Labtech). Percentage inhibition values at a single concentration or enzyme inhibition (IC50) values are determined from those curves. One skilled in the art will appreciate that the values generated either as percentage inhibition at a single concentration or IC50 values are subject to experimental variation.
693
Total Activities
229
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Ubiquitin-like modifier-activating enzyme ATG7 (CHEMBL2321621) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
ATG7 inhibitors and the uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 231 | 7.05 | 7.46 |
| kon | 231 | - | - |
| k_off | 231 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4465490 | — | — | 3 | 7.46 |
| CHEMBL4449861 | — | — | 3 | 7.46 |
| CHEMBL5801088 | — | — | 3 | 7.46 |
| CHEMBL4521754 | — | — | 3 | 7.46 |
| CHEMBL4535927 | — | — | 3 | 7.46 |
| CHEMBL4579107 | — | — | 3 | 7.46 |
| CHEMBL4577562 | — | — | 3 | 7.46 |
| CHEMBL4476015 | — | — | 3 | 7.46 |
| CHEMBL4451885 | — | — | 3 | 7.46 |
| CHEMBL4439106 | — | — | 3 | 7.46 |
| CHEMBL4531796 | — | — | 3 | 7.46 |
| CHEMBL4471670 | — | — | 3 | 7.46 |
| CHEMBL4473245 | — | — | 3 | 7.46 |
| CHEMBL4453903 | — | — | 3 | 7.46 |
| CHEMBL4548069 | — | — | 3 | 7.46 |
| CHEMBL4450880 | — | — | 3 | 7.46 |
| CHEMBL4539952 | — | — | 3 | 7.46 |
| CHEMBL4476094 | — | — | 3 | 7.46 |
| CHEMBL4586427 | — | — | 3 | 7.46 |
| CHEMBL4455332 | — | — | 3 | 7.46 |
| CHEMBL4589701 | — | — | 3 | 7.46 |
| CHEMBL4551253 | — | — | 3 | 7.46 |
| CHEMBL4529186 | — | — | 3 | 7.46 |
| CHEMBL4532634 | — | — | 3 | 7.46 |
| CHEMBL4517771 | — | — | 3 | 7.46 |
| CHEMBL4574054 | — | — | 3 | 7.46 |
| CHEMBL4545152 | — | — | 3 | 7.46 |
| CHEMBL4551395 | — | — | 3 | 7.46 |
| CHEMBL4436997 | — | — | 3 | 7.46 |
| CHEMBL4542158 | — | — | 3 | 7.46 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452757 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4449861 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4551253 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4466430 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4543610 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4589701 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4549926 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4455332 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4521754 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4557103 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4439106 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4557469 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4586427 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4576658 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4475447 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4476094 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4539952 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4453903 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4526319 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4589617 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4518269 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4518410 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4476516 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5927711 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4471670 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4558671 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4476015 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4551395 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4545152 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4436997 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5801088 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4464322 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4449596 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4517065 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4574054 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4483085 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4444895 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4451885 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4577562 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4542158 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4469119 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4471077 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4469589 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4467807 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4517771 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4457043 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4532634 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4447381 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4454053 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4529186 | — | IC50 | = | 35.0 | nM | 7.46 |