Assay Detail
Binding
CHEMBL4620359
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Inhibition of recombinant human TDO expressed in Escherichia coli BL21 using L-Trp as substrate incubated for 30 mins by enzymatic 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
Synthesis of novel tryptanthrin derivatives as dual inhibitors of indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.21 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4645973 | — | — | 1 | 7.52 |
| CHEMBL4643029 | — | — | 1 | 7.22 |
| CHEMBL4647345 | — | — | 1 | 6.75 |
| CHEMBL4646483 | — | — | 1 | 6.52 |
| CHEMBL4648181 | — | — | 1 | 6.43 |
| CHEMBL4633682 | — | — | 1 | 6.38 |
| CHEMBL4646657 | — | — | 1 | 6.35 |
| CHEMBL4645897 | — | — | 1 | 6.00 |
| CHEMBL4644380 | — | — | 1 | 5.95 |
| CHEMBL4635512 | — | — | 1 | 5.92 |
| CHEMBL4643729 | — | — | 1 | 5.54 |
| CHEMBL4644195 | — | — | 1 | 5.22 |
| CHEMBL1812545 | — | — | 1 | 4.94 |
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4645973 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4643029 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4647345 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4646483 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4648181 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4633682 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4646657 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4645897 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL4644380 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL4635512 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4643729 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL4644195 | — | IC50 | = | 6020.0 | nM | 5.22 |
| CHEMBL1812545 | — | IC50 | = | 11580.0 | nM | 4.94 |
| CHEMBL3545369 | EPACADOSTAT | IC50 | - | — | - |