Assay Detail
Binding
CHEMBL890258
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Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Hep 3B2 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha (CHEMBL2221345) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.68 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | 2.0 | 1 | 7.21 |
| CHEMBL388964 | SIBIRIQUINONE A | — | 1 | 6.55 |
| CHEMBL187460 | CRYPTOTANSHINONE | — | 1 | 5.87 |
| CHEMBL227075 | DIHYDROTANSHINONE I | — | 1 | 5.64 |
| CHEMBL227074 | SIBIRIQUINONE B | — | 1 | 5.50 |
| CHEMBL187266 | TANSHINONE IIA | — | 1 | 5.21 |
| CHEMBL2146517 | METHYL TANSHINONATE | — | 1 | 5.13 |
| CHEMBL363535 | TANSHINONE I | — | 1 | 5.07 |
| CHEMBL227129 | 12-DEOXYTANSHINQUINONE B | — | 1 | 4.97 |
| CHEMBL227128 | DIHYDROISOTANSHINONE II | — | 1 | - |
| CHEMBL227131 | ISOTANSHINONE II | — | 1 | - |
| CHEMBL227130 | NEOCRYPTOTANSHINONE | — | 1 | - |
| CHEMBL390741 | DANSHENXINKUN A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383824 | ALVESPIMYCIN | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL388964 | SIBIRIQUINONE A | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL187460 | CRYPTOTANSHINONE | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL227075 | DIHYDROTANSHINONE I | IC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL227074 | SIBIRIQUINONE B | IC50 | = | 3180.0 | nM | 5.50 |
| CHEMBL187266 | TANSHINONE IIA | IC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL2146517 | METHYL TANSHINONATE | IC50 | = | 7340.0 | nM | 5.13 |
| CHEMBL363535 | TANSHINONE I | IC50 | = | 8510.0 | nM | 5.07 |
| CHEMBL227129 | 12-DEOXYTANSHINQUINONE B | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL227128 | DIHYDROISOTANSHINONE II | IC50 | > | 20000.0 | nM | - |
| CHEMBL227131 | ISOTANSHINONE II | IC50 | > | 20000.0 | nM | - |
| CHEMBL227130 | NEOCRYPTOTANSHINONE | IC50 | > | 20000.0 | nM | - |
| CHEMBL390741 | DANSHENXINKUN A | IC50 | > | 20000.0 | nM | - |