Assay Detail
Binding
CHEMBL4482019
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Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of 2,5-dimethylfuran-3-carboxylic acid derivatives as potential IDO1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.18 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4562263 | — | — | 1 | 8.34 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 8.25 |
| CHEMBL4591635 | — | — | 1 | 8.24 |
| CHEMBL4535597 | — | — | 1 | 8.23 |
| CHEMBL4593106 | — | — | 1 | 8.18 |
| CHEMBL4555117 | — | — | 1 | 8.13 |
| CHEMBL4548296 | — | — | 1 | 8.09 |
| CHEMBL4217909 | — | — | 1 | 7.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4562263 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4591635 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4535597 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4593106 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4555117 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL4548296 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL4217909 | — | IC50 | = | 10.7 | nM | 7.97 |