Assay Detail
Functional
CHEMBL908782
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Inhibition of HDAC activity measured by HDAC Fluorescent Activity Assay (mean of two experiments)
25
Total Activities
25
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-(1H-pyrazol-3-yl)-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.63 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL218511 | — | — | 1 | 8.30 |
| CHEMBL217004 | — | — | 1 | 8.30 |
| CHEMBL216249 | — | — | 1 | 8.22 |
| CHEMBL216625 | — | — | 1 | 8.22 |
| CHEMBL386473 | — | — | 1 | 8.15 |
| CHEMBL426343 | — | — | 1 | 8.10 |
| CHEMBL216248 | — | — | 1 | 8.10 |
| CHEMBL217098 | — | — | 1 | 8.05 |
| CHEMBL217186 | — | — | 1 | 7.96 |
| CHEMBL386752 | — | — | 1 | 7.92 |
| CHEMBL384961 | — | — | 1 | 7.89 |
| CHEMBL385852 | — | — | 1 | 7.72 |
| CHEMBL217468 | — | — | 1 | 7.70 |
| CHEMBL385406 | — | — | 1 | 7.68 |
| CHEMBL218514 | — | — | 1 | 7.66 |
| CHEMBL217716 | — | — | 1 | 7.54 |
| CHEMBL386135 | — | — | 1 | 7.48 |
| CHEMBL218080 | — | — | 1 | 7.47 |
| CHEMBL217029 | — | — | 1 | 7.32 |
| CHEMBL216499 | — | — | 1 | 7.16 |
| CHEMBL216359 | — | — | 1 | 7.00 |
| CHEMBL217604 | — | — | 1 | 6.97 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 6.90 |
| CHEMBL218236 | — | — | 1 | 6.82 |
| CHEMBL216885 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL218511 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL217004 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL216249 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL216625 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL386473 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL426343 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL216248 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL217098 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL217186 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL386752 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL384961 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL385852 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL217468 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL385406 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL218514 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL217716 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL386135 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL218080 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL217029 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL216499 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL216359 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL217604 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL218236 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL216885 | — | IC50 | = | 750.0 | nM | 6.12 |