Assay Detail
Binding
CHEMBL4359028
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IDO1 in IFNgamma-stimulated human A375 cells assessed as reduction in L-Kyn level measured after 48 hrs by HPLC 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
Discovery of Highly Potent Benzimidazole Derivatives as Indoleamine 2,3-Dioxygenase-1 (IDO1) Inhibitors: From Structure-Based Virtual Screening to in Vivo Pharmacodynamic Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.82 | 8.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545369 | EPACADOSTAT | 3.0 | 1 | 8.11 |
| CHEMBL4557994 | — | — | 1 | 7.80 |
| CHEMBL4571131 | — | — | 1 | 7.72 |
| CHEMBL4448402 | — | — | 1 | 7.14 |
| CHEMBL4458549 | — | — | 1 | 7.05 |
| CHEMBL4466117 | — | — | 1 | 6.87 |
| CHEMBL4531545 | — | — | 1 | 6.49 |
| CHEMBL4472707 | — | — | 1 | 6.39 |
| CHEMBL4588288 | — | — | 1 | 6.38 |
| CHEMBL4451614 | — | — | 1 | 6.32 |
| CHEMBL4443904 | — | — | 1 | 6.20 |
| CHEMBL4439258 | — | — | 1 | 6.11 |
| CHEMBL4457663 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545369 | EPACADOSTAT | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL4557994 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4571131 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4448402 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4458549 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4466117 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4531545 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL4472707 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL4588288 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4451614 | — | IC50 | = | 477.0 | nM | 6.32 |
| CHEMBL4443904 | — | IC50 | = | 636.0 | nM | 6.20 |
| CHEMBL4439258 | — | IC50 | = | 781.0 | nM | 6.11 |
| CHEMBL4457663 | — | IC50 | = | 961.0 | nM | 6.02 |