Assay Detail
Binding
CHEMBL3872639
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Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U-87MG ATCC |
| 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 | 5.09 | 6.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432537 | — | — | 1 | 6.35 |
| CHEMBL1098875 | — | — | 1 | 5.92 |
| CHEMBL72165 | — | — | 1 | 5.50 |
| CHEMBL306946 | TRYPTANTHRIN | — | 1 | 5.30 |
| CHEMBL3087009 | — | — | 1 | 5.09 |
| CHEMBL1276265 | — | — | 1 | 4.74 |
| CHEMBL3087010 | — | — | 1 | 4.71 |
| CHEMBL312537 | — | — | 1 | 4.66 |
| CHEMBL3086870 | — | — | 1 | 4.42 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | — | 1 | 4.25 |
| CHEMBL571209 | INDOXIMOD | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432537 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1098875 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL72165 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL306946 | TRYPTANTHRIN | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3087009 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL1276265 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL3087010 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL312537 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL3086870 | — | IC50 | = | 37800.0 | nM | 4.42 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | IC50 | = | 56900.0 | nM | 4.25 |
| CHEMBL571209 | INDOXIMOD | IC50 | = | 148900.0 | nM | - |