Assay Detail
Binding
CHEMBL4709781
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TDO (unknown origin) assessed as reduction in L-kynurenine formation using L-tryptophan as substrate incubated for 30 mins 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 | 7.30 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4787695 | — | — | 1 | 8.40 |
| CHEMBL4765090 | — | — | 1 | 8.00 |
| CHEMBL4756155 | — | — | 1 | 7.85 |
| CHEMBL4780314 | — | — | 1 | 7.82 |
| CHEMBL4747779 | — | — | 1 | 7.82 |
| CHEMBL4791729 | — | — | 1 | 7.75 |
| CHEMBL4753714 | — | — | 1 | 7.75 |
| CHEMBL4798028 | — | — | 1 | 7.68 |
| CHEMBL4783665 | — | — | 1 | 7.60 |
| CHEMBL4642346 | — | — | 1 | 7.60 |
| CHEMBL4785841 | — | — | 1 | 7.60 |
| CHEMBL4777219 | — | — | 1 | 7.55 |
| CHEMBL4763934 | — | — | 1 | 7.47 |
| CHEMBL4753565 | — | — | 1 | 7.47 |
| CHEMBL4749726 | — | — | 1 | 7.44 |
| CHEMBL3628599 | — | — | 1 | 7.44 |
| CHEMBL4783159 | — | — | 1 | 7.38 |
| CHEMBL4741094 | — | — | 1 | 7.32 |
| CHEMBL4741069 | — | — | 1 | 7.32 |
| CHEMBL4748868 | — | — | 1 | 7.31 |
| CHEMBL4762048 | — | — | 1 | 7.24 |
| CHEMBL4756754 | — | — | 1 | 7.19 |
| CHEMBL4752502 | — | — | 1 | 7.18 |
| CHEMBL4300931 | — | — | 1 | 7.16 |
| CHEMBL4648447 | — | — | 1 | 7.15 |
| CHEMBL4759518 | — | — | 1 | 7.00 |
| CHEMBL4750649 | — | — | 1 | 6.98 |
| CHEMBL4786114 | — | — | 1 | 6.98 |
| CHEMBL4763470 | — | — | 1 | 6.88 |
| CHEMBL4751532 | — | — | 1 | 6.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4787695 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4765090 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4756155 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4780314 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4747779 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4791729 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4753714 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4798028 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4783665 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4642346 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4785841 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4777219 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4763934 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4753565 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3628599 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4749726 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4783159 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4741094 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4741069 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4748868 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4762048 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4756754 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4752502 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4300931 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4648447 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4759518 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL4750649 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL4786114 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL4763470 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4751532 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4762733 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4747007 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL3628551 | — | IC50 | = | 712.0 | nM | 6.15 |
| CHEMBL1644447 | — | IC50 | = | 858.0 | nM | 6.07 |
| CHEMBL4748072 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3545369 | EPACADOSTAT | IC50 | > | 10000.0 | nM | - |
| CHEMBL4751793 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4798525 | — | IC50 | > | 10000.0 | nM | - |