Assay Detail
Binding
CHEMBL3379482
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Inhibition of HDAC8 (unknown origin) using fluorogenic tetrapeptide RHK(Ac)K(Ac) substrate by fluorescence assay
34
Total Activities
34
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
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.51 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3356935 | — | — | 1 | 8.05 |
| CHEMBL3356937 | — | — | 1 | 7.77 |
| CHEMBL3356933 | — | — | 1 | 7.64 |
| CHEMBL3356925 | — | — | 1 | 7.40 |
| CHEMBL3356918 | — | — | 1 | 7.23 |
| CHEMBL3356929 | — | — | 1 | 7.21 |
| CHEMBL3356527 | — | — | 1 | 7.21 |
| CHEMBL3356924 | — | — | 1 | 7.00 |
| CHEMBL3356923 | — | — | 1 | 6.97 |
| CHEMBL3356524 | — | — | 1 | 6.97 |
| CHEMBL3356922 | — | — | 1 | 6.97 |
| CHEMBL3356915 | — | — | 1 | 6.91 |
| CHEMBL3356916 | — | — | 1 | 6.87 |
| CHEMBL3356526 | — | — | 1 | 6.70 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.61 |
| CHEMBL3356936 | — | — | 1 | 6.61 |
| CHEMBL3356919 | — | — | 1 | 6.55 |
| CHEMBL3356927 | — | — | 1 | 6.51 |
| CHEMBL3353927 | — | — | 1 | 6.50 |
| CHEMBL3356917 | — | — | 1 | 6.44 |
| CHEMBL3356932 | — | — | 1 | 6.43 |
| CHEMBL3356523 | — | — | 1 | 6.38 |
| CHEMBL3356931 | — | — | 1 | 6.35 |
| CHEMBL3356921 | — | — | 1 | 6.26 |
| CHEMBL3356934 | — | — | 1 | 6.04 |
| CHEMBL325676 | — | — | 1 | 5.97 |
| CHEMBL326433 | 8-MERCAPTO-OCTANOIC ACID PHENYLAMIDE | — | 1 | 5.95 |
| CHEMBL109654 | — | — | 1 | 5.87 |
| CHEMBL3356926 | — | — | 1 | 5.69 |
| CHEMBL3356939 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3356935 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3356937 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3356933 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3356925 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3356918 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3356929 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3356527 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL3356924 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL3356923 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3356524 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL3356922 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL3356915 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3356916 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3356526 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3356936 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL3356919 | — | IC50 | = | 281.0 | nM | 6.55 |
| CHEMBL3356927 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3353927 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL3356917 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3356932 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL3356523 | — | IC50 | = | 416.0 | nM | 6.38 |
| CHEMBL3356931 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3356921 | — | IC50 | = | 545.0 | nM | 6.26 |
| CHEMBL3356934 | — | IC50 | = | 904.0 | nM | 6.04 |
| CHEMBL325676 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL326433 | 8-MERCAPTO-OCTANOIC ACID PHENYLAMIDE | IC50 | = | 1120.0 | nM | 5.95 |
| CHEMBL109654 | — | IC50 | = | 1360.0 | nM | 5.87 |
| CHEMBL3356926 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL3356939 | — | IC50 | = | 2230.0 | nM | 5.65 |
| CHEMBL3356930 | — | IC50 | = | 2330.0 | nM | 5.63 |
| CHEMBL3356928 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL3356920 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL213934 | — | IC50 | = | 44000.0 | nM | 4.36 |