Assay Detail
Binding
CHEMBL4356125
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Inhibition of recombinant human TDO expressed in Escherichia coli BL21 (DE3) assessed as reduction in conversion of L-tryptophan to N-formyl kynurenine using L-tryptophan as substrate after 30 mins by methylene blue assay
14
Total Activities
14
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 |
|---|---|---|---|
| IC50 | 14 | 5.59 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4452150 | — | — | 1 | 6.39 |
| CHEMBL4577825 | — | — | 1 | 6.35 |
| CHEMBL4437046 | — | — | 1 | 6.12 |
| CHEMBL4436480 | — | — | 1 | 6.06 |
| CHEMBL4588805 | — | — | 1 | 6.06 |
| CHEMBL4545004 | — | — | 1 | 5.62 |
| CHEMBL4536439 | — | — | 1 | 5.59 |
| CHEMBL4471831 | — | — | 1 | 5.50 |
| CHEMBL4468741 | — | — | 1 | 5.42 |
| CHEMBL4584081 | — | — | 1 | 5.19 |
| CHEMBL4471895 | — | — | 1 | 5.17 |
| CHEMBL4578338 | — | — | 1 | 5.00 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 4.19 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4452150 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4577825 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4437046 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4436480 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4588805 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL4545004 | — | IC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL4536439 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL4471831 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4468741 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL4584081 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4471895 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL4578338 | — | IC50 | = | 10090.0 | nM | 5.00 |
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 64500.0 | nM | 4.19 |
| CHEMBL504816 | (L)-1-METHYLTRYPTOPHAN | IC50 | - | — | - |