Assay Detail
Binding
CHEMBL4622407
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDO1 in human whole blood stimulated with IFNgamma/LPS using L-tryptophan/kynurenine as substrate incubated for 15 mins prior to IFNgamma/LPS stimulation and further incubated for 18 hrs followed by isotope labeled L-tryptophan/kynurenine addition on day 2 by LC/MS-MS analysis
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.90 | 7.52 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4638223 | — | — | 1 | 7.52 |
| CHEMBL4644751 | — | — | 2 | 7.44 |
| CHEMBL4632992 | — | — | 1 | 6.92 |
| CHEMBL4648765 | — | — | 1 | 6.90 |
| CHEMBL4642946 | — | — | 1 | 6.86 |
| CHEMBL4647172 | — | — | 1 | 6.85 |
| CHEMBL4639353 | — | — | 1 | 6.81 |
| CHEMBL4638557 | — | — | 1 | 6.76 |
| CHEMBL4647108 | — | — | 1 | 6.56 |
| CHEMBL4641517 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4638223 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4644751 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4632992 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4648765 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4642946 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL4647172 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4639353 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL4638557 | — | IC50 | = | 174.0 | nM | 6.76 |
| CHEMBL4647108 | — | IC50 | = | 276.0 | nM | 6.56 |
| CHEMBL4641517 | — | IC50 | = | 443.0 | nM | 6.35 |
| CHEMBL4644751 | — | IC90 | = | 912.0 | nM | - |