Assay Detail
Binding
CHEMBL5355891
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Inhibition of human recombinant HDAC8 using fluorogenic diacetylated p53 (379-382 residues) (RHKK(Ac)K(Ac)AMC) as substrate
25
Total Activities
25
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
Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.53 | 7.33 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4550522 | — | — | 1 | 7.33 |
| CHEMBL5408688 | — | — | 1 | 6.98 |
| CHEMBL5400896 | — | — | 1 | 6.78 |
| CHEMBL5429873 | — | — | 1 | 6.74 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.51 |
| CHEMBL3426804 | — | — | 1 | 6.21 |
| CHEMBL5425559 | — | — | 1 | 6.05 |
| CHEMBL5418060 | — | — | 1 | 6.02 |
| CHEMBL5426896 | — | — | 1 | 6.01 |
| CHEMBL5401106 | — | — | 1 | 6.00 |
| CHEMBL4435005 | — | — | 1 | 5.96 |
| CHEMBL5411948 | — | — | 1 | 5.96 |
| CHEMBL4521590 | — | — | 1 | 5.74 |
| CHEMBL5396543 | — | — | 1 | 4.50 |
| CHEMBL5412379 | — | — | 1 | 4.45 |
| CHEMBL5396691 | — | — | 1 | 4.37 |
| CHEMBL5433683 | — | — | 1 | 4.18 |
| CHEMBL5399910 | — | — | 1 | 4.12 |
| CHEMBL5414244 | — | — | 1 | 4.11 |
| CHEMBL5419832 | — | — | 1 | 4.11 |
| CHEMBL5429446 | — | — | 1 | 4.01 |
| CHEMBL5417858 | — | — | 1 | - |
| CHEMBL5420814 | — | — | 1 | - |
| CHEMBL5409567 | — | — | 1 | - |
| CHEMBL5409409 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4550522 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5408688 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5400896 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL5429873 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL3426804 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL5425559 | — | IC50 | = | 882.0 | nM | 6.05 |
| CHEMBL5418060 | — | IC50 | = | 964.0 | nM | 6.02 |
| CHEMBL5426896 | — | IC50 | = | 976.0 | nM | 6.01 |
| CHEMBL5401106 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4435005 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL5411948 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4521590 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL5396543 | — | IC50 | = | 31400.0 | nM | 4.50 |
| CHEMBL5412379 | — | IC50 | = | 35600.0 | nM | 4.45 |
| CHEMBL5396691 | — | IC50 | = | 43100.0 | nM | 4.37 |
| CHEMBL5433683 | — | IC50 | = | 66200.0 | nM | 4.18 |
| CHEMBL5399910 | — | IC50 | = | 75200.0 | nM | 4.12 |
| CHEMBL5414244 | — | IC50 | = | 77100.0 | nM | 4.11 |
| CHEMBL5419832 | — | IC50 | = | 77100.0 | nM | 4.11 |
| CHEMBL5429446 | — | IC50 | = | 98400.0 | nM | 4.01 |
| CHEMBL5417858 | — | IC50 | - | — | - | |
| CHEMBL5420814 | — | IC50 | - | — | - | |
| CHEMBL5409567 | — | IC50 | - | — | - | |
| CHEMBL5409409 | — | IC50 | - | — | - |