Assay Detail
Binding
CHEMBL4124444
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 FITC-HIF1-alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay
34
Total Activities
34
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 | 34 | 6.39 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4127286 | — | — | 1 | 8.72 |
| CHEMBL4129555 | — | — | 1 | 7.28 |
| CHEMBL4126434 | — | — | 1 | 7.21 |
| CHEMBL4125856 | — | — | 1 | 7.21 |
| CHEMBL4128320 | — | — | 1 | 7.17 |
| CHEMBL4127232 | — | — | 1 | 7.12 |
| CHEMBL4126256 | — | — | 1 | 7.10 |
| CHEMBL4129832 | — | — | 1 | 6.64 |
| CHEMBL4129725 | — | — | 1 | 6.64 |
| CHEMBL4128470 | — | — | 1 | 6.61 |
| CHEMBL4128884 | — | — | 1 | 6.57 |
| CHEMBL4126407 | — | — | 1 | 6.55 |
| CHEMBL4129500 | — | — | 1 | 6.55 |
| CHEMBL4126047 | — | — | 1 | 6.51 |
| CHEMBL4126204 | — | — | 1 | 6.43 |
| CHEMBL4128943 | — | — | 1 | 6.38 |
| CHEMBL4129697 | — | — | 1 | 6.38 |
| CHEMBL4128469 | — | — | 1 | 6.38 |
| CHEMBL4129898 | — | — | 1 | 6.38 |
| CHEMBL4127429 | — | — | 1 | 6.24 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 6.23 |
| CHEMBL4127491 | — | — | 1 | 6.22 |
| CHEMBL4127542 | — | — | 1 | 6.12 |
| CHEMBL4127340 | — | — | 1 | 6.10 |
| CHEMBL4129131 | — | — | 1 | 6.07 |
| CHEMBL4128767 | — | — | 1 | 6.07 |
| CHEMBL4129696 | — | — | 1 | 6.00 |
| CHEMBL4126684 | — | — | 1 | 5.82 |
| CHEMBL4127631 | — | — | 1 | 5.67 |
| CHEMBL4126257 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4127286 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4129555 | — | IC50 | = | 52.84 | nM | 7.28 |
| CHEMBL4126434 | — | IC50 | = | 62.23 | nM | 7.21 |
| CHEMBL4125856 | — | IC50 | = | 61.08 | nM | 7.21 |
| CHEMBL4128320 | — | IC50 | = | 67.58 | nM | 7.17 |
| CHEMBL4127232 | — | IC50 | = | 75.82 | nM | 7.12 |
| CHEMBL4126256 | — | IC50 | = | 79.69 | nM | 7.10 |
| CHEMBL4129725 | — | IC50 | = | 228.2 | nM | 6.64 |
| CHEMBL4129832 | — | IC50 | = | 231.1 | nM | 6.64 |
| CHEMBL4128470 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4128884 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL4126407 | — | IC50 | = | 278.3 | nM | 6.55 |
| CHEMBL4129500 | — | IC50 | = | 280.6 | nM | 6.55 |
| CHEMBL4126047 | — | IC50 | = | 308.3 | nM | 6.51 |
| CHEMBL4126204 | — | IC50 | = | 375.4 | nM | 6.43 |
| CHEMBL4129697 | — | IC50 | = | 418.7 | nM | 6.38 |
| CHEMBL4128469 | — | IC50 | = | 418.3 | nM | 6.38 |
| CHEMBL4128943 | — | IC50 | = | 418.3 | nM | 6.38 |
| CHEMBL4129898 | — | IC50 | = | 419.3 | nM | 6.38 |
| CHEMBL4127429 | — | IC50 | = | 579.7 | nM | 6.24 |
| CHEMBL2338329 | ROXADUSTAT | IC50 | = | 591.4 | nM | 6.23 |
| CHEMBL4127491 | — | IC50 | = | 608.2 | nM | 6.22 |
| CHEMBL4127542 | — | IC50 | = | 759.4 | nM | 6.12 |
| CHEMBL4127340 | — | IC50 | = | 801.4 | nM | 6.10 |
| CHEMBL4128767 | — | IC50 | = | 853.8 | nM | 6.07 |
| CHEMBL4129131 | — | IC50 | = | 853.8 | nM | 6.07 |
| CHEMBL4129696 | — | IC50 | = | 995.8 | nM | 6.00 |
| CHEMBL4126684 | — | IC50 | = | 1507.0 | nM | 5.82 |
| CHEMBL4127631 | — | IC50 | = | 2165.0 | nM | 5.67 |
| CHEMBL4126257 | — | IC50 | = | 2291.0 | nM | 5.64 |
| CHEMBL4128670 | — | IC50 | = | 3086.0 | nM | 5.51 |
| CHEMBL4127086 | — | IC50 | = | 3594.0 | nM | 5.44 |
| CHEMBL4128528 | — | IC50 | = | 5527.0 | nM | 5.26 |
| CHEMBL4129956 | — | IC50 | = | 6995.0 | nM | 5.16 |