Assay Detail
Binding
CHEMBL4356124
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Inhibition of C-terminal His6-tagged human IDO2 (14 to 420 residues) 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 dye based microplate reader analysis
13
Total Activities
13
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 | 13 | 4.41 | 4.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 4.99 |
| CHEMBL4452150 | — | — | 1 | 4.85 |
| CHEMBL4437046 | — | — | 1 | 4.73 |
| CHEMBL4436480 | — | — | 1 | 4.50 |
| CHEMBL4588805 | — | — | 1 | 4.40 |
| CHEMBL4578338 | — | — | 1 | 4.40 |
| CHEMBL4471831 | — | — | 1 | 4.38 |
| CHEMBL4545004 | — | — | 1 | 4.33 |
| CHEMBL4536439 | — | — | 1 | 4.33 |
| CHEMBL4577825 | — | — | 1 | 4.20 |
| CHEMBL4584081 | — | — | 1 | 4.10 |
| CHEMBL4471895 | — | — | 1 | 4.08 |
| CHEMBL4468741 | — | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 10340.0 | nM | 4.99 |
| CHEMBL4452150 | — | IC50 | = | 14030.0 | nM | 4.85 |
| CHEMBL4437046 | — | IC50 | = | 18440.0 | nM | 4.73 |
| CHEMBL4436480 | — | IC50 | = | 31450.0 | nM | 4.50 |
| CHEMBL4588805 | — | IC50 | = | 39550.0 | nM | 4.40 |
| CHEMBL4578338 | — | IC50 | = | 40090.0 | nM | 4.40 |
| CHEMBL4471831 | — | IC50 | = | 41630.0 | nM | 4.38 |
| CHEMBL4545004 | — | IC50 | = | 46860.0 | nM | 4.33 |
| CHEMBL4536439 | — | IC50 | = | 46820.0 | nM | 4.33 |
| CHEMBL4577825 | — | IC50 | = | 62610.0 | nM | 4.20 |
| CHEMBL4584081 | — | IC50 | = | 79910.0 | nM | 4.10 |
| CHEMBL4471895 | — | IC50 | = | 82570.0 | nM | 4.08 |
| CHEMBL4468741 | — | IC50 | = | 91350.0 | nM | 4.04 |