Assay Detail
Binding
CHEMBL5738951
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The present invention provides a novel class of demethylase FTO inhibitors which inhibit FTO protein activity at very low concentration (typically IC50 values is below 30 μM).
57
Total Activities
16
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
Alpha-ketoglutarate-dependent dioxygenase FTO (CHEMBL2331065) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
2-(substituted benzene matrix) aromatic formate FTO inhibitor, preparation method therefor, and applications thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.59 | 7.22 |
| kon | 19 | - | - |
| k_off | 19 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4572939 | — | — | 12 | 7.22 |
| CHEMBL4532629 | — | — | 3 | 6.40 |
| CHEMBL4870546 | — | — | 3 | 6.16 |
| CHEMBL4862027 | — | — | 3 | - |
| CHEMBL4521076 | — | — | 3 | - |
| CHEMBL4471728 | — | — | 3 | - |
| CHEMBL4563561 | — | — | 3 | - |
| CHEMBL4567838 | — | — | 3 | - |
| CHEMBL4442310 | — | — | 3 | - |
| CHEMBL6012039 | — | — | 3 | - |
| CHEMBL5596599 | — | — | 3 | - |
| CHEMBL5926785 | — | — | 3 | - |
| CHEMBL5872559 | — | — | 3 | - |
| CHEMBL5969087 | — | — | 3 | - |
| CHEMBL5894854 | — | — | 3 | - |
| CHEMBL5182230 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4572939 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4532629 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4870546 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5182230 | — | IC50 | < | 5000.0 | nM | - |
| CHEMBL4567838 | — | k_off | = | - | s-1 | - |
| CHEMBL5182230 | — | kon | = | - | — | - |
| CHEMBL5182230 | — | k_off | = | - | s-1 | - |
| CHEMBL4563561 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4870546 | — | kon | = | - | — | - |
| CHEMBL4870546 | — | k_off | = | - | s-1 | - |
| CHEMBL4862027 | — | IC50 | < | 5000.0 | nM | - |
| CHEMBL4862027 | — | kon | = | - | — | - |
| CHEMBL4862027 | — | k_off | = | - | s-1 | - |
| CHEMBL4521076 | — | IC50 | < | 5000.0 | nM | - |
| CHEMBL4521076 | — | kon | = | - | — | - |
| CHEMBL4521076 | — | k_off | = | - | s-1 | - |
| CHEMBL4471728 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4471728 | — | kon | = | - | — | - |
| CHEMBL4471728 | — | k_off | = | - | s-1 | - |
| CHEMBL4572939 | — | kon | = | - | — | - |
| CHEMBL4572939 | — | k_off | = | - | s-1 | - |
| CHEMBL4572939 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4563561 | — | kon | = | - | — | - |
| CHEMBL4563561 | — | k_off | = | - | s-1 | - |
| CHEMBL4567838 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4567838 | — | kon | = | - | — | - |
| CHEMBL5596599 | — | k_off | = | - | s-1 | - |
| CHEMBL5926785 | — | kon | = | - | — | - |
| CHEMBL4572939 | — | kon | = | - | — | - |
| CHEMBL4572939 | — | k_off | = | - | s-1 | - |
| CHEMBL4572939 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4572939 | — | kon | = | - | — | - |
| CHEMBL4572939 | — | k_off | = | - | s-1 | - |
| CHEMBL6012039 | — | IC50 | < | 5000.0 | nM | - |
| CHEMBL6012039 | — | kon | = | - | — | - |
| CHEMBL6012039 | — | k_off | = | - | s-1 | - |
| CHEMBL5596599 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL5596599 | — | kon | = | - | — | - |
| CHEMBL5894854 | — | k_off | = | - | s-1 | - |
| CHEMBL5926785 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL4572939 | — | kon | = | - | — | - |
| CHEMBL5926785 | — | k_off | = | - | s-1 | - |
| CHEMBL5872559 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL5872559 | — | kon | = | - | — | - |
| CHEMBL5872559 | — | k_off | = | - | s-1 | - |
| CHEMBL5969087 | — | IC50 | < | 1000.0 | nM | - |
| CHEMBL5969087 | — | kon | = | - | — | - |
| CHEMBL5969087 | — | k_off | = | - | s-1 | - |
| CHEMBL5894854 | — | IC50 | < | 5000.0 | nM | - |
| CHEMBL5894854 | — | kon | = | - | — | - |