Assay Detail
Binding
CHEMBL3872637
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Inhibition of recombinant human C-terminal His6-tagged IDO2 (14-420 residues) expressed in Escherichia coli BL21(DE3) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate after 30 mins in presence of catalase by methylene blue dye based assay
11
Total Activities
11
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 |
Publication
Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 4.67 | 5.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432537 | — | — | 1 | 5.75 |
| CHEMBL1098875 | — | — | 1 | 5.12 |
| CHEMBL72165 | — | — | 1 | 5.08 |
| CHEMBL306946 | TRYPTANTHRIN | — | 1 | 4.76 |
| CHEMBL3087009 | — | — | 1 | 4.66 |
| CHEMBL312537 | — | — | 1 | 4.50 |
| CHEMBL3087010 | — | — | 1 | 4.36 |
| CHEMBL3086870 | — | — | 1 | 4.25 |
| CHEMBL1276265 | — | — | 1 | 4.17 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | — | 1 | 4.08 |
| CHEMBL571209 | INDOXIMOD | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432537 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1098875 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL72165 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL306946 | TRYPTANTHRIN | IC50 | = | 17300.0 | nM | 4.76 |
| CHEMBL3087009 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL312537 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL3087010 | — | IC50 | = | 43400.0 | nM | 4.36 |
| CHEMBL3086870 | — | IC50 | = | 56800.0 | nM | 4.25 |
| CHEMBL1276265 | — | IC50 | = | 67900.0 | nM | 4.17 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | IC50 | = | 82500.0 | nM | 4.08 |
| CHEMBL571209 | INDOXIMOD | IC50 | = | 262700.0 | nM | - |