Assay Detail
Binding
CHEMBL3705564
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: Hydroxylated HIF bonds specifically to the von Hippel-Lindau protein-elongin B-elongin C complex (VBC complex). This interaction occurs only if HIF is hydroxylated on a conserved prolyl radical. It is the basis for the biochemical determination of HIF prolyl hydroxylase activity. The test is carried out as described [Oehme F., Jonghaus W., Narouz-Ott L., Huetter J., Flamme I., Anal. Biochem. 330 (1), 74-80 (2004)].
20
Total Activities
20
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
Substituted dihydropyrazolones for treating cardiovascular and hematological diseases
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.15 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3646117 | — | — | 1 | 7.30 |
| CHEMBL3646120 | — | — | 1 | 6.72 |
| CHEMBL3646107 | — | — | 1 | 6.47 |
| CHEMBL3646123 | — | — | 1 | 6.46 |
| CHEMBL3646125 | — | — | 1 | 6.44 |
| CHEMBL3646118 | MOLIDUSTAT | 2.0 | 1 | 6.31 |
| CHEMBL3646108 | — | — | 1 | 6.30 |
| CHEMBL3646110 | — | — | 1 | 6.25 |
| CHEMBL3646126 | — | — | 1 | 6.16 |
| CHEMBL3646124 | — | — | 1 | 6.13 |
| CHEMBL3646109 | — | — | 1 | 6.12 |
| CHEMBL3646112 | — | — | 1 | 6.11 |
| CHEMBL3646116 | — | — | 1 | 5.96 |
| CHEMBL3646115 | — | — | 1 | 5.85 |
| CHEMBL3646113 | — | — | 1 | 5.85 |
| CHEMBL3646122 | — | — | 1 | 5.77 |
| CHEMBL3646111 | — | — | 1 | 5.75 |
| CHEMBL3646119 | — | — | 1 | 5.72 |
| CHEMBL3646114 | — | — | 1 | 5.70 |
| CHEMBL3646121 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3646117 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3646120 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3646107 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL3646123 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3646125 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3646118 | MOLIDUSTAT | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3646108 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3646110 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3646126 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL3646124 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3646109 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3646112 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3646116 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3646115 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3646113 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3646122 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3646111 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3646119 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3646114 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3646121 | — | IC50 | = | 2800.0 | nM | 5.55 |