Assay Detail
Binding
CHEMBL5216103
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 expressed in Escherichia coli BL21 (DE3) incubated for 10 mins using 15-mer ssRNA oligonucleotide [AUUGUGG(m6A)-CUGCAGC as substrate by SPE-MS-based assay
9
Total Activities
9
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 | 9 | 5.85 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5219846 | — | — | 1 | 7.10 |
| CHEMBL5220094 | — | — | 1 | 6.48 |
| CHEMBL5219336 | — | — | 1 | 6.37 |
| CHEMBL5220148 | — | — | 1 | 6.10 |
| CHEMBL5219099 | — | — | 1 | 6.05 |
| CHEMBL5220246 | — | — | 1 | 5.85 |
| CHEMBL5220431 | — | — | 1 | 5.29 |
| CHEMBL5219135 | — | — | 1 | 4.82 |
| CHEMBL5218469 | — | — | 1 | 4.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5219846 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5220094 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5219336 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5220148 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL5219099 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5220246 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5220431 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5219135 | — | IC50 | = | 15200.0 | nM | 4.82 |
| CHEMBL5218469 | — | IC50 | = | 26000.0 | nM | 4.58 |