Assay Detail
Functional
CHEMBL908805
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Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments)
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.45 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL217246 | — | — | 1 | 8.40 |
| CHEMBL387447 | — | — | 1 | 8.22 |
| CHEMBL386914 | — | — | 1 | 8.15 |
| CHEMBL218392 | — | — | 1 | 8.15 |
| CHEMBL216463 | — | — | 1 | 8.10 |
| CHEMBL385562 | — | — | 1 | 8.10 |
| CHEMBL441699 | — | — | 1 | 8.10 |
| CHEMBL217615 | — | — | 1 | 8.05 |
| CHEMBL436964 | — | — | 1 | 8.05 |
| CHEMBL217881 | — | — | 1 | 8.05 |
| CHEMBL216300 | — | — | 1 | 8.05 |
| CHEMBL217097 | — | — | 1 | 8.05 |
| CHEMBL217882 | — | — | 1 | 7.96 |
| CHEMBL387247 | — | — | 1 | 7.96 |
| CHEMBL217531 | — | — | 1 | 7.92 |
| CHEMBL216301 | — | — | 1 | 7.92 |
| CHEMBL384733 | — | — | 1 | 7.89 |
| CHEMBL216896 | — | — | 1 | 7.85 |
| CHEMBL216884 | — | — | 1 | 7.80 |
| CHEMBL263570 | — | — | 1 | 7.80 |
| CHEMBL385934 | — | — | 1 | 7.77 |
| CHEMBL217529 | — | — | 1 | 7.75 |
| CHEMBL217716 | — | — | 1 | 7.54 |
| CHEMBL387105 | — | — | 1 | 7.52 |
| CHEMBL279353 | — | — | 1 | 7.51 |
| CHEMBL217093 | — | — | 1 | 7.46 |
| CHEMBL425971 | — | — | 1 | 7.10 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.90 |
| CHEMBL217817 | — | — | 1 | 6.73 |
| CHEMBL216509 | — | — | 1 | 6.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL217246 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL387447 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL218392 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL386914 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL216463 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL385562 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL441699 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL216300 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL217097 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL217881 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL436964 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL217615 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL217882 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL387247 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL216301 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL217531 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL384733 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL216896 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL216884 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL263570 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL385934 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL217529 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL217716 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL387105 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL279353 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL217093 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL425971 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL217817 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL216509 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL385404 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL217871 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL216885 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL217573 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL216292 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL217816 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL217750 | — | IC50 | = | 2500.0 | nM | 5.60 |