Assay Detail
Binding
CHEMBL4356135
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Uncompetitive inhibition of recombinant human TDO expressed in Escherichia coli BL21 (DE3) assessed as assessed as inhibition constant using varying concentration of L-tryptophan as substrate by Dixon plot analysis
9
Total Activities
9
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
N-Benzyl/Aryl Substituted Tryptanthrin as Dual Inhibitors of Indoleamine 2,3-Dioxygenase and Tryptophan 2,3-Dioxygenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 5.83 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436480 | — | — | 1 | 6.92 |
| CHEMBL4437046 | — | — | 1 | 6.51 |
| CHEMBL4588805 | — | — | 1 | 6.47 |
| CHEMBL4468741 | — | — | 1 | 5.91 |
| CHEMBL4578338 | — | — | 1 | 5.81 |
| CHEMBL4584081 | — | — | 1 | 5.63 |
| CHEMBL4471895 | — | — | 1 | 4.75 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 4.66 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436480 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4437046 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4588805 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4468741 | — | Ki | = | 1240.0 | nM | 5.91 |
| CHEMBL4578338 | — | Ki | = | 1560.0 | nM | 5.81 |
| CHEMBL4584081 | — | Ki | = | 2360.0 | nM | 5.63 |
| CHEMBL4471895 | — | Ki | = | 17960.0 | nM | 4.75 |
| CHEMBL3545369 | EPACADOSTAT | Ki | = | 21700.0 | nM | 4.66 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | Ki | - | — | - |