Assay Detail
Binding
CHEMBL924307
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Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human Hep3B cells by reporter gene assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Hep 3B2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.55 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219673 | — | — | 1 | 6.40 |
| CHEMBL430393 | — | — | 1 | 6.00 |
| CHEMBL399636 | — | — | 1 | 5.92 |
| CHEMBL373396 | — | — | 1 | 5.58 |
| CHEMBL249027 | — | — | 1 | 5.51 |
| CHEMBL249023 | — | — | 1 | 5.47 |
| CHEMBL249028 | — | — | 1 | 5.23 |
| CHEMBL403789 | — | — | 1 | 4.95 |
| CHEMBL333985 | — | — | 1 | 4.86 |
| CHEMBL401390 | — | — | 1 | - |
| CHEMBL250671 | — | — | 1 | - |
| CHEMBL248836 | — | — | 1 | - |
| CHEMBL248650 | — | — | 1 | - |
| CHEMBL399845 | — | — | 1 | - |
| CHEMBL248835 | — | — | 1 | - |
| CHEMBL398897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219673 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL430393 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL399636 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL373396 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL249027 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL249023 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL249028 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL403789 | — | IC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL333985 | — | IC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL401390 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL250671 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL248836 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL248650 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL399845 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL248835 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL398897 | — | IC50 | > | 30000.0 | nM | - |