Assay Detail
Binding
CHEMBL3089095
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Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.16 | 10.74 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL432537 | — | — | 1 | 10.74 |
| CHEMBL1098875 | — | — | 1 | 7.64 |
| CHEMBL3087012 | — | — | 1 | 7.61 |
| CHEMBL3087010 | — | — | 1 | 7.57 |
| CHEMBL306946 | TRYPTANTHRIN | — | 1 | 7.27 |
| CHEMBL72165 | — | — | 1 | 7.27 |
| CHEMBL1276265 | — | — | 1 | 6.74 |
| CHEMBL3087014 | — | — | 1 | 6.73 |
| CHEMBL3087009 | — | — | 1 | 6.33 |
| CHEMBL2314972 | — | — | 1 | 6.11 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | — | 1 | 4.74 |
| CHEMBL312537 | — | — | 1 | - |
| CHEMBL3086870 | — | — | 1 | - |
| CHEMBL3087011 | — | — | 1 | - |
| CHEMBL3087013 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL432537 | — | IC50 | = | 0.018 | nM | 10.74 |
| CHEMBL1098875 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3087012 | — | IC50 | = | 24.3 | nM | 7.61 |
| CHEMBL3087010 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL306946 | TRYPTANTHRIN | IC50 | = | 53.7 | nM | 7.27 |
| CHEMBL72165 | — | IC50 | = | 53.9 | nM | 7.27 |
| CHEMBL1276265 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3087014 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL3087009 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL2314972 | — | IC50 | = | 779.0 | nM | 6.11 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL312537 | — | IC50 | - | — | - | |
| CHEMBL3086870 | — | IC50 | - | — | - | |
| CHEMBL3087011 | — | IC50 | - | — | - | |
| CHEMBL3087013 | — | Inhibition | - | % | - |