Assay Detail
Binding
CHEMBL5539985
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Inhibition of PHD2 (unknown origin) preincubated for 30 mins followed by substrate addition and measured after 30 mins by HTS plate reader analysis
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
Discovery of Novel and Potent Prolyl Hydroxylase Domain-Containing Protein (PHD) Inhibitors for The Treatment of Anemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 8.09 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5572635 | — | — | 1 | 9.00 |
| CHEMBL5590779 | — | — | 1 | 9.00 |
| CHEMBL5564592 | — | — | 1 | 8.70 |
| CHEMBL5574218 | — | — | 1 | 8.70 |
| CHEMBL5565890 | — | — | 1 | 8.70 |
| CHEMBL5563061 | — | — | 1 | 8.60 |
| CHEMBL5572587 | — | — | 1 | 8.52 |
| CHEMBL5575448 | — | — | 1 | 8.40 |
| CHEMBL5572628 | — | — | 1 | 8.40 |
| CHEMBL5594033 | — | — | 1 | 8.40 |
| CHEMBL5567289 | — | — | 1 | 8.05 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 7.85 |
| CHEMBL5571964 | — | — | 1 | 7.72 |
| CHEMBL5562929 | — | — | 1 | 7.43 |
| CHEMBL5583677 | — | — | 1 | 7.06 |
| CHEMBL5594247 | — | — | 1 | 6.54 |
| CHEMBL5572863 | — | — | 1 | 6.53 |
| CHEMBL5572357 | — | — | 1 | - |
| CHEMBL5570245 | — | — | 1 | - |
| CHEMBL5572667 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5572635 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5590779 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5564592 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5574218 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5565890 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5563061 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5572587 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5575448 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5572628 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5594033 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5567289 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2338329 | ROXADUSTAT | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5571964 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5562929 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5583677 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5594247 | — | IC50 | = | 291.0 | nM | 6.54 |
| CHEMBL5572863 | — | IC50 | = | 297.0 | nM | 6.53 |
| CHEMBL5572357 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5570245 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL5572667 | — | IC50 | > | 2000.0 | nM | - |