Assay Detail
Binding
CHEMBL4329410
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TDO expressed in human T-REx cells using L-tryptophan as substrate after 20 hrs
28
Total Activities
28
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
Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 4.93 | 5.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4582341 | — | — | 1 | 5.46 |
| CHEMBL4446245 | — | — | 1 | 5.41 |
| CHEMBL4544399 | — | — | 1 | 5.36 |
| CHEMBL4440040 | — | — | 1 | 5.34 |
| CHEMBL4468826 | — | — | 1 | 5.34 |
| CHEMBL4578334 | — | — | 1 | 5.32 |
| CHEMBL4516705 | — | — | 1 | 5.29 |
| CHEMBL4558294 | — | — | 1 | 5.25 |
| CHEMBL4473408 | — | — | 1 | 5.24 |
| CHEMBL4544607 | — | — | 1 | 5.21 |
| CHEMBL4585829 | — | — | 1 | 5.20 |
| CHEMBL4517541 | — | — | 1 | 5.15 |
| CHEMBL4561507 | — | — | 1 | 5.09 |
| CHEMBL4571508 | — | — | 1 | 5.04 |
| CHEMBL4519297 | — | — | 1 | 4.87 |
| CHEMBL4438707 | — | — | 1 | 4.72 |
| CHEMBL4539097 | — | — | 1 | 4.66 |
| CHEMBL4451390 | — | — | 1 | 4.65 |
| CHEMBL4524223 | — | — | 1 | 4.62 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 4.60 |
| CHEMBL4439774 | — | — | 1 | 4.53 |
| CHEMBL4435742 | — | — | 1 | 4.31 |
| CHEMBL4455554 | — | — | 1 | 4.30 |
| CHEMBL4443640 | — | — | 1 | 4.23 |
| CHEMBL4440269 | — | — | 1 | 4.11 |
| CHEMBL4590292 | — | — | 1 | - |
| CHEMBL4086143 | PF-06840003 | 1.0 | 1 | - |
| CHEMBL4468567 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4582341 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL4446245 | — | IC50 | = | 3920.0 | nM | 5.41 |
| CHEMBL4544399 | — | IC50 | = | 4410.0 | nM | 5.36 |
| CHEMBL4440040 | — | IC50 | = | 4530.0 | nM | 5.34 |
| CHEMBL4468826 | — | IC50 | = | 4540.0 | nM | 5.34 |
| CHEMBL4578334 | — | IC50 | = | 4820.0 | nM | 5.32 |
| CHEMBL4516705 | — | IC50 | = | 5150.0 | nM | 5.29 |
| CHEMBL4558294 | — | IC50 | = | 5620.0 | nM | 5.25 |
| CHEMBL4473408 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4544607 | — | IC50 | = | 6210.0 | nM | 5.21 |
| CHEMBL4585829 | — | IC50 | = | 6370.0 | nM | 5.20 |
| CHEMBL4517541 | — | IC50 | = | 7150.0 | nM | 5.15 |
| CHEMBL4561507 | — | IC50 | = | 8110.0 | nM | 5.09 |
| CHEMBL4571508 | — | IC50 | = | 9020.0 | nM | 5.04 |
| CHEMBL4519297 | — | IC50 | = | 13600.0 | nM | 4.87 |
| CHEMBL4438707 | — | IC50 | = | 19100.0 | nM | 4.72 |
| CHEMBL4539097 | — | IC50 | = | 21800.0 | nM | 4.66 |
| CHEMBL4451390 | — | IC50 | = | 22500.0 | nM | 4.65 |
| CHEMBL4524223 | — | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 25200.0 | nM | 4.60 |
| CHEMBL4439774 | — | IC50 | = | 29800.0 | nM | 4.53 |
| CHEMBL4435742 | — | IC50 | = | 48800.0 | nM | 4.31 |
| CHEMBL4455554 | — | IC50 | = | 49700.0 | nM | 4.30 |
| CHEMBL4443640 | — | IC50 | = | 58700.0 | nM | 4.23 |
| CHEMBL4440269 | — | IC50 | = | 77400.0 | nM | 4.11 |
| CHEMBL4590292 | — | IC50 | = | 123000.0 | nM | - |
| CHEMBL4086143 | PF-06840003 | IC50 | = | 378000.0 | nM | - |
| CHEMBL4468567 | — | IC50 | = | 2770000.0 | nM | - |