Assay Detail
Binding
CHEMBL4124447
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HIF-PHD2 (181 to 426 residues) (unknown origin) using HIF1-alpha (556 to 574 residues) as substrate in presence of 2-OG preincubated for 30 mins followed by OPD addition measured after 10 mins by fluorescence assay
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
Click Chemistry-Based Discovery of [3-Hydroxy-5-(1 H-1,2,3-triazol-4-yl)picolinoyl]glycines as Orally Active Hypoxia-Inducing Factor Prolyl Hydroxylase Inhibitors with Favorable Safety Profiles for the Treatment of Anemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.26 | 5.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126434 | — | — | 1 | 5.88 |
| CHEMBL4129555 | — | — | 1 | 5.56 |
| CHEMBL4128320 | — | — | 1 | 5.27 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 5.24 |
| CHEMBL4125856 | — | — | 1 | 5.21 |
| CHEMBL4126256 | — | — | 1 | 5.19 |
| CHEMBL4127232 | — | — | 1 | 5.16 |
| CHEMBL4129725 | — | — | 1 | 5.09 |
| CHEMBL4129131 | — | — | 1 | 4.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126434 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL4129555 | — | IC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL4128320 | — | IC50 | = | 5340.0 | nM | 5.27 |
| CHEMBL2338329 | ROXADUSTAT | IC50 | = | 5740.0 | nM | 5.24 |
| CHEMBL4125856 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL4126256 | — | IC50 | = | 6430.0 | nM | 5.19 |
| CHEMBL4127232 | — | IC50 | = | 6880.0 | nM | 5.16 |
| CHEMBL4129725 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL4129131 | — | IC50 | = | 17060.0 | nM | 4.77 |