Assay Detail
Binding
CHEMBL3776331
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged full-length FIH (unknown origin) expressed in Escherichia coli Rosetta 2(DE3)pLysS using SMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN peptide/100 uM alpha-ketoglutarate as substrate/cofactor incubated for 45 mins by MALDI assay
6
Total Activities
6
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 |
Target
Hypoxia-inducible factor 1-alpha inhibitor (CHEMBL5909) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 4.20 | 5.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316034 | — | — | 1 | 5.07 |
| CHEMBL3775867 | — | — | 1 | 3.33 |
| CHEMBL3775262 | — | — | 1 | - |
| CHEMBL3775272 | — | — | 1 | - |
| CHEMBL3775380 | — | — | 1 | - |
| CHEMBL3774598 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316034 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL3775867 | — | IC50 | = | 473000.0 | nM | 3.33 |
| CHEMBL3775262 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3775272 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3775380 | — | IC50 | > | 500000.0 | nM | - |
| CHEMBL3774598 | — | IC50 | > | 500000.0 | nM | - |