Assay Detail
Binding
CHEMBL4362337
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TrxR1 (unknown origin) using DTNB as substrate preincubated for 30 mins in presence of insulin followed by substrate addition by colorimetry
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 |
Target
Thioredoxin reductase 1, cytoplasmic (CHEMBL1927) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel electrophilic amides amenable by the Ugi reaction perturb thioredoxin system via thioredoxin reductase 1 (TrxR1) inhibition: Identification of DVD-445 as a new lead compound for anticancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.72 | 6.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4577957 | — | — | 1 | 6.12 |
| CHEMBL4562297 | — | — | 1 | 6.09 |
| CHEMBL4459518 | — | — | 1 | 6.02 |
| CHEMBL4589636 | — | — | 1 | 5.60 |
| CHEMBL4451049 | — | — | 1 | 5.28 |
| CHEMBL4452177 | — | — | 1 | 5.18 |
| CHEMBL4544484 | — | — | 1 | - |
| CHEMBL4443061 | — | — | 1 | - |
| CHEMBL4447931 | — | — | 1 | - |
| CHEMBL4515694 | — | — | 1 | - |
| CHEMBL4460514 | — | — | 1 | - |
| CHEMBL4465914 | — | — | 1 | - |
| CHEMBL4439743 | — | — | 1 | - |
| CHEMBL465843 | PIPLARTINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4577957 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL4562297 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4459518 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4589636 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4451049 | — | IC50 | = | 5280.0 | nM | 5.28 |
| CHEMBL4452177 | — | IC50 | = | 6610.0 | nM | 5.18 |
| CHEMBL4544484 | — | IC50 | - | — | - | |
| CHEMBL4443061 | — | IC50 | - | — | - | |
| CHEMBL4447931 | — | IC50 | - | — | - | |
| CHEMBL4515694 | — | IC50 | - | — | - | |
| CHEMBL4460514 | — | IC50 | - | — | - | |
| CHEMBL4465914 | — | IC50 | - | — | - | |
| CHEMBL4439743 | — | IC50 | - | — | - | |
| CHEMBL465843 | PIPLARTINE | IC50 | - | — | - |