Assay Detail
Binding
CHEMBL1042996
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Inhibition of N-terminal his-tagged human indoleamine 2,3-dioxygenase expressed in Escherichia coli assessed as N'-formylkynurenine formation by spectrophotometry
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.07 | 7.23 |
| Ki | 1 | 5.96 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565923 | — | — | 1 | 7.23 |
| CHEMBL584991 | — | — | 1 | 7.17 |
| CHEMBL565488 | — | — | 1 | 7.14 |
| CHEMBL579014 | — | — | 1 | 7.07 |
| CHEMBL573690 | — | — | 1 | 6.37 |
| CHEMBL567225 | — | — | 1 | 6.30 |
| CHEMBL565489 | — | — | 1 | 6.26 |
| CHEMBL585186 | — | — | 1 | 5.96 |
| CHEMBL567441 | — | — | 1 | 5.85 |
| CHEMBL574139 | — | — | 1 | 5.68 |
| CHEMBL577494 | — | — | 1 | 5.50 |
| CHEMBL568287 | — | — | 1 | 5.36 |
| CHEMBL573686 | — | — | 1 | 5.22 |
| CHEMBL576019 | — | — | 1 | 5.19 |
| CHEMBL577067 | — | — | 1 | 4.60 |
| CHEMBL584992 | — | — | 1 | - |
| CHEMBL565924 | — | — | 1 | - |
| CHEMBL567442 | — | — | 1 | - |
| CHEMBL567317 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565923 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL584991 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL565488 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL579014 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL573690 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL567225 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL565489 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL585186 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL567441 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL574139 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL577494 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL568287 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL573686 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL576019 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL577067 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL584992 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL565924 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL567442 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL567317 | — | IC50 | > | 20000.0 | nM | - |