Assay Detail
Binding
CHEMBL1174248
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of dehydrogenase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of geraniol dehydrogenation in presence of saturating concentration of NADP+
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Aldo-keto reductase family 1 member B10 (CHEMBL5983) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.98 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1172665 | — | — | 1 | 8.57 |
| CHEMBL1171546 | — | — | 1 | 7.92 |
| CHEMBL1169756 | — | — | 1 | 7.80 |
| CHEMBL1169757 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1172665 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL1171546 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1169756 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1169757 | — | Ki | = | 24.0 | nM | 7.62 |