Assay Detail
Binding
CHEMBL2183271
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Inhibition of HIF1alpha in human HCT116 cells under hypoxic condition after 16 hrs by dual luciferase reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.74 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2178399 | — | — | 1 | 6.92 |
| CHEMBL2178407 | — | — | 1 | 6.13 |
| CHEMBL2178416 | — | — | 1 | 6.09 |
| CHEMBL2178409 | — | — | 1 | 5.98 |
| CHEMBL2178404 | — | — | 1 | 5.97 |
| CHEMBL2178414 | — | — | 1 | 5.93 |
| CHEMBL2178419 | — | — | 1 | 5.87 |
| CHEMBL2178403 | — | — | 1 | 5.87 |
| CHEMBL2178417 | — | — | 1 | 5.74 |
| CHEMBL2178405 | — | — | 1 | 5.73 |
| CHEMBL2178410 | — | — | 1 | 5.66 |
| CHEMBL2178415 | — | — | 1 | 5.62 |
| CHEMBL427092 | — | — | 1 | 5.61 |
| CHEMBL2177118 | — | — | 1 | 5.59 |
| CHEMBL2178418 | — | — | 1 | 5.58 |
| CHEMBL2178411 | — | — | 1 | 5.38 |
| CHEMBL373396 | — | — | 1 | 5.30 |
| CHEMBL2178408 | — | — | 1 | 5.22 |
| CHEMBL2178406 | — | — | 1 | 4.80 |
| CHEMBL2178412 | — | — | 1 | - |
| CHEMBL2178413 | — | — | 1 | - |
| CHEMBL2178402 | — | — | 1 | - |
| CHEMBL2178401 | — | — | 1 | - |
| CHEMBL2178400 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2178399 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2178407 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL2178416 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2178409 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL2178404 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL2178414 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL2178419 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL2178403 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL2178417 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL2178405 | — | IC50 | = | 1850.0 | nM | 5.73 |
| CHEMBL2178410 | — | IC50 | = | 2170.0 | nM | 5.66 |
| CHEMBL2178415 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL427092 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL2177118 | — | IC50 | = | 2540.0 | nM | 5.59 |
| CHEMBL2178418 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL2178411 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL373396 | — | IC50 | = | 5030.0 | nM | 5.30 |
| CHEMBL2178408 | — | IC50 | = | 6030.0 | nM | 5.22 |
| CHEMBL2178406 | — | IC50 | = | 15750.0 | nM | 4.80 |
| CHEMBL2178412 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2178413 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2178402 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2178401 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2178400 | — | IC50 | > | 20000.0 | nM | - |