Assay Detail
Binding
CHEMBL5502163
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Inhibition of HIF-1 (unknown origin) expressed in MH7A cells cotransfected with HRE and renilla luciferase assessed as reduction in luminescence signal preincubated for 1 hr under normoxic condition followed by 24 hrs incubation under hypoxic condition by dual luciferase reporter assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MH7A |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.58 | 6.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5517764 | — | — | 1 | 6.26 |
| CHEMBL5558890 | — | — | 1 | 6.09 |
| CHEMBL5557368 | — | — | 1 | 6.04 |
| CHEMBL5556834 | — | — | 1 | 5.84 |
| CHEMBL5537041 | — | — | 1 | 5.66 |
| CHEMBL5559433 | — | — | 1 | 5.48 |
| CHEMBL5555700 | — | — | 1 | 5.45 |
| CHEMBL4447149 | — | — | 1 | 5.34 |
| CHEMBL5557934 | — | — | 1 | 5.23 |
| CHEMBL5517981 | — | — | 1 | 5.21 |
| CHEMBL5523621 | — | — | 1 | 5.17 |
| CHEMBL5517668 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5517764 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5558890 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5557368 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL5556834 | — | IC50 | = | 1460.0 | nM | 5.84 |
| CHEMBL5537041 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL5559433 | — | IC50 | = | 3310.0 | nM | 5.48 |
| CHEMBL5555700 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL4447149 | — | IC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL5557934 | — | IC50 | = | 5920.0 | nM | 5.23 |
| CHEMBL5517981 | — | IC50 | = | 6210.0 | nM | 5.21 |
| CHEMBL5523621 | — | IC50 | = | 6730.0 | nM | 5.17 |
| CHEMBL5517668 | — | IC50 | = | 7390.0 | nM | 5.13 |