Assay Detail
Binding
CHEMBL5216102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length N-terminal hexahistidine-tagged human FTO demethylation activity expressed in Escherichia coli BL21 (DE3) incubated for 30 mins using 5-mer ssRNA oligonucleotide [GG(m6A)CU] as substrate by LCMS-based assay
12
Total Activities
12
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 |
Target
Alpha-ketoglutarate-dependent dioxygenase FTO (CHEMBL2331065) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Design of Selective Fat Mass and Obesity Associated Protein (FTO) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 4.95 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5219846 | — | — | 1 | 5.82 |
| CHEMBL5218636 | — | — | 1 | 5.64 |
| CHEMBL5219099 | — | — | 1 | 5.24 |
| CHEMBL5219336 | — | — | 1 | 5.21 |
| CHEMBL5220148 | — | — | 1 | 5.16 |
| CHEMBL5219491 | — | — | 1 | 4.96 |
| CHEMBL5220094 | — | — | 1 | 4.91 |
| CHEMBL5173876 | — | — | 1 | 4.90 |
| CHEMBL5219989 | — | — | 1 | 4.63 |
| CHEMBL5219094 | — | — | 1 | 4.45 |
| CHEMBL5220246 | — | — | 1 | 4.26 |
| CHEMBL5220431 | — | — | 1 | 4.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5219846 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL5218636 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5219099 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL5219336 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5220148 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL5219491 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL5220094 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL5173876 | — | IC50 | = | 12500.0 | nM | 4.90 |
| CHEMBL5219989 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL5219094 | — | IC50 | = | 35200.0 | nM | 4.45 |
| CHEMBL5220246 | — | IC50 | = | 54500.0 | nM | 4.26 |
| CHEMBL5220431 | — | IC50 | = | 60200.0 | nM | 4.22 |