Assay Detail
Binding
CHEMBL924308
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Inhibition of hypoxia induced HIF1-alpha transcriptional activity in human AGS 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 | AGS |
| 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 | 5.58 | 6.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219673 | — | — | 1 | 6.46 |
| CHEMBL373396 | — | — | 1 | 6.16 |
| CHEMBL430393 | — | — | 1 | 6.10 |
| CHEMBL401390 | — | — | 1 | 6.05 |
| CHEMBL248836 | — | — | 1 | 5.89 |
| CHEMBL249027 | — | — | 1 | 5.75 |
| CHEMBL333985 | — | — | 1 | 5.70 |
| CHEMBL399636 | — | — | 1 | 5.70 |
| CHEMBL249028 | — | — | 1 | 5.30 |
| CHEMBL249023 | — | — | 1 | 5.28 |
| CHEMBL403789 | — | — | 1 | 4.96 |
| CHEMBL248835 | — | — | 1 | 4.73 |
| CHEMBL248650 | — | — | 1 | 4.52 |
| CHEMBL250671 | — | — | 1 | - |
| CHEMBL399845 | — | — | 1 | - |
| CHEMBL398897 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219673 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL373396 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL430393 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL401390 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL248836 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL249027 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL333985 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL399636 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL249028 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL249023 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL403789 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL248835 | — | IC50 | = | 18600.0 | nM | 4.73 |
| CHEMBL248650 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL250671 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL399845 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL398897 | — | IC50 | > | 30000.0 | nM | - |