Assay Detail
Binding
CHEMBL3705129
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Inhibition Assay: In vitro tests for determination of the activity and selectivity of HIF prolyl 4-hydroxylase inhibitors. 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)].
9
Total Activities
9
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 and their use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.61 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3115317 | — | — | 1 | 7.16 |
| CHEMBL3640646 | — | — | 1 | 7.05 |
| CHEMBL3640645 | — | — | 1 | 6.89 |
| CHEMBL3642645 | — | — | 1 | 6.77 |
| CHEMBL3642643 | — | — | 1 | 6.75 |
| CHEMBL3642644 | — | — | 1 | 6.42 |
| CHEMBL3640643 | — | — | 1 | 6.27 |
| CHEMBL3640644 | — | — | 1 | 6.12 |
| CHEMBL3640642 | — | — | 1 | 6.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3115317 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3640646 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3640645 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3642645 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL3642643 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3642644 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3640643 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3640644 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3640642 | — | IC50 | = | 880.0 | nM | 6.06 |