Assay Detail
Binding
CHEMBL3129509
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Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.21 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1836142 | THAILANDEPSIN A | — | 1 | 9.00 |
| CHEMBL3126833 | — | — | 1 | 8.92 |
| CHEMBL343448 | ROMIDEPSIN | 4.0 | 1 | 8.44 |
| CHEMBL3126831 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1836142 | THAILANDEPSIN A | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3126833 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL343448 | ROMIDEPSIN | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3126831 | — | IC50 | = | 336.6 | nM | 6.47 |