Assay Detail
Binding
CHEMBL2423478
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Inhibition of recombinant human HDAC1 enzyme using flurogenic Ac-LeuGlyLys (Ac)-AMC as substrate after 15 to 30 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Total synthesis and full histone deacetylase inhibitory profiling of Azumamides A-E as well as β²- epi-Azumamide E and β³-epi-Azumamide E.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.02 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 8.10 |
| CHEMBL257972 | AZUMAMIDE C | — | 1 | 7.50 |
| CHEMBL402363 | AZUMAMIDE E | — | 1 | 7.17 |
| CHEMBL402727 | AZUMAMIDE B | — | 1 | 5.30 |
| CHEMBL343448 | ROMIDEPSIN | 4.0 | 1 | - |
| CHEMBL257973 | AZUMAMIDE D | — | 1 | - |
| CHEMBL255714 | AZUMAMIDE A | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL98 | VORINOSTAT | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL257972 | AZUMAMIDE C | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL402363 | AZUMAMIDE E | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL402727 | AZUMAMIDE B | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL343448 | ROMIDEPSIN | Ki | = | 0.002 | nM | - |
| CHEMBL257973 | AZUMAMIDE D | Ki | > | 5000.0 | nM | - |
| CHEMBL255714 | AZUMAMIDE A | Ki | > | 5000.0 | nM | - |