Assay Detail
Binding
CHEMBL5735292
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Indoleamine-2,3-Dioxygenase 1 Inhibitory Activity: Experimental method: IDO-1 can oxidatively cleave the indole ring of tryptophan to form N-formylkynurenine. Referring to the method in the literature (Eddy W. Yue, et al. J. Med. Chem. 2009, 52, 7364-7367), 20 nM IDO-1, 2 mM D-tryptophan, 20 mM ascorbic acid, 3.5M methyl blue and 0.2 mg/mL antioxidant enzyme were sequentially added to 50 mM potassium phosphate buffer at room temperature. Due to the formation of N-formylkynurenine, the reaction rate was recorded by the increasing absorbance of the solution at 321 nm. IC50 values were calculated using Prism GraphPad software.
126
Total Activities
36
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Use of aza-tryptanthrin derivatives as inhibitors of IDO1 and/or TDO
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 6.63 | 8.26 |
| kon | 42 | - | - |
| k_off | 42 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL584991 | — | — | 3 | 8.26 |
| CHEMBL365701 | — | — | 6 | 8.26 |
| CHEMBL5950956 | — | — | 3 | 8.26 |
| CHEMBL5896110 | — | — | 3 | 8.26 |
| CHEMBL187652 | — | — | 6 | 8.26 |
| CHEMBL5977622 | — | — | 3 | 8.26 |
| CHEMBL5856042 | — | — | 3 | 8.26 |
| CHEMBL2347793 | — | — | 3 | 8.26 |
| CHEMBL2347776 | — | — | 3 | 8.26 |
| CHEMBL5880422 | — | — | 3 | 8.26 |
| CHEMBL5824667 | — | — | 6 | 6.26 |
| CHEMBL1098875 | — | — | 3 | 6.26 |
| CHEMBL5985313 | — | — | 6 | 6.26 |
| CHEMBL432537 | — | — | 3 | 6.26 |
| CHEMBL5903836 | — | — | 3 | 6.26 |
| CHEMBL5967303 | — | — | 3 | 6.26 |
| CHEMBL5932991 | — | — | 6 | 6.26 |
| CHEMBL6003894 | — | — | 3 | 6.26 |
| CHEMBL5743808 | — | — | 3 | 6.26 |
| CHEMBL5956469 | — | — | 3 | 6.26 |
| CHEMBL5783618 | — | — | 3 | 6.26 |
| CHEMBL6029347 | — | — | 3 | 6.26 |
| CHEMBL6022429 | — | — | 3 | 6.26 |
| CHEMBL5810711 | — | — | 3 | 6.26 |
| CHEMBL1098826 | — | — | 6 | 6.26 |
| CHEMBL5820407 | — | — | 3 | 6.26 |
| CHEMBL306946 | TRYPTANTHRIN | — | 3 | 5.26 |
| CHEMBL5941164 | — | — | 3 | 5.26 |
| CHEMBL5962154 | — | — | 3 | 5.26 |
| CHEMBL5909424 | — | — | 3 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5950956 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL584991 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5977622 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2347793 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL365701 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL187652 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL2347776 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5856042 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL365701 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL187652 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5896110 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5880422 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL5820407 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1098826 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5810711 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5903836 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6029347 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5824667 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL432537 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5932991 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5985313 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5967303 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6022429 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1098875 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5985313 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5783618 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5824667 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5743808 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5932991 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5956469 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1098826 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL6003894 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5952261 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL6045556 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5962154 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5909424 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5857619 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5799295 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5869900 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5941164 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL306946 | TRYPTANTHRIN | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL5783618 | — | k_off | = | - | s-1 | - |
| CHEMBL5909424 | — | kon | = | - | — | - |
| CHEMBL5783618 | — | kon | = | - | — | - |
| CHEMBL6022429 | — | kon | = | - | — | - |
| CHEMBL6022429 | — | k_off | = | - | s-1 | - |
| CHEMBL5880422 | — | k_off | = | - | s-1 | - |
| CHEMBL5896110 | — | kon | = | - | — | - |
| CHEMBL5880422 | — | kon | = | - | — | - |
| CHEMBL584991 | — | kon | = | - | — | - |