Assay Detail
Binding
CHEMBL4709780
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDO1 (unknown origin) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate incubated for 30 mins by microplate spectrophotometry analysis
38
Total Activities
38
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
Discovery and structure-activity relationship studies of 1-aryl-1H-naphtho[2,3-d][1,2,3]triazole-4,9-dione derivatives as potent dual inhibitors of indoleamine 2,3-dioxygenase 1 (IDO1) and trytophan 2,3-dioxygenase (TDO).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 7.26 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787695 | — | — | 1 | 8.30 |
| CHEMBL4765090 | — | — | 1 | 8.00 |
| CHEMBL4756155 | — | — | 1 | 7.89 |
| CHEMBL4747779 | — | — | 1 | 7.82 |
| CHEMBL4791729 | — | — | 1 | 7.70 |
| CHEMBL4780314 | — | — | 1 | 7.64 |
| CHEMBL4753714 | — | — | 1 | 7.64 |
| CHEMBL4798028 | — | — | 1 | 7.64 |
| CHEMBL4752502 | — | — | 1 | 7.58 |
| CHEMBL4642346 | — | — | 1 | 7.57 |
| CHEMBL4777219 | — | — | 1 | 7.54 |
| CHEMBL4741069 | — | — | 1 | 7.52 |
| CHEMBL4785841 | — | — | 1 | 7.52 |
| CHEMBL4741094 | — | — | 1 | 7.48 |
| CHEMBL4753565 | — | — | 1 | 7.48 |
| CHEMBL4762048 | — | — | 1 | 7.47 |
| CHEMBL4749726 | — | — | 1 | 7.40 |
| CHEMBL4763934 | — | — | 1 | 7.40 |
| CHEMBL4783159 | — | — | 1 | 7.35 |
| CHEMBL4759518 | — | — | 1 | 7.28 |
| CHEMBL4748868 | — | — | 1 | 7.24 |
| CHEMBL4783665 | — | — | 1 | 7.22 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 7.12 |
| CHEMBL4750649 | — | — | 1 | 7.11 |
| CHEMBL4763470 | — | — | 1 | 7.09 |
| CHEMBL4300931 | — | — | 1 | 7.00 |
| CHEMBL4762733 | — | — | 1 | 6.95 |
| CHEMBL4648447 | — | — | 1 | 6.94 |
| CHEMBL4756754 | — | — | 1 | 6.91 |
| CHEMBL4751532 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787695 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4765090 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4756155 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4747779 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4791729 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4780314 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4753714 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4798028 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4752502 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4642346 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4777219 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4741069 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4785841 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4741094 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4753565 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4762048 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4749726 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4763934 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4783159 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4759518 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4748868 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4783665 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4750649 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4763470 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4300931 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4762733 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4648447 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4756754 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4751532 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4786114 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4747007 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL3628599 | — | IC50 | = | 658.0 | nM | 6.18 |
| CHEMBL3628551 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL1644447 | — | IC50 | = | 886.0 | nM | 6.05 |
| CHEMBL4798525 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4751793 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4748072 | — | IC50 | > | 10000.0 | nM | - |