Assay Detail
Binding
CHEMBL4340709
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Inhibition of recombinant human PHD2 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by LC-MS analysis
10
Total Activities
10
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
Inhibition of a viral prolyl hydroxylase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.45 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3646117 | — | — | 1 | 8.52 |
| CHEMBL3646118 | MOLIDUSTAT | 2.0 | 1 | 8.15 |
| CHEMBL2338329 | ROXADUSTAT | 4.0 | 1 | 7.57 |
| CHEMBL3646221 | VADADUSTAT | 4.0 | 1 | 7.54 |
| CHEMBL4163812 | — | — | 1 | 7.17 |
| CHEMBL316034 | — | — | 1 | 5.16 |
| CHEMBL90852 | N-OXALYLGLYCINE | — | 1 | 5.10 |
| CHEMBL1230640 | — | — | 1 | 4.84 |
| CHEMBL3785164 | — | — | 1 | 4.02 |
| CHEMBL4540977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3646117 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3646118 | MOLIDUSTAT | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2338329 | ROXADUSTAT | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3646221 | VADADUSTAT | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4163812 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL316034 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL90852 | N-OXALYLGLYCINE | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL1230640 | — | IC50 | = | 14300.0 | nM | 4.84 |
| CHEMBL3785164 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL4540977 | — | IC50 | > | 100000.0 | nM | - |