Assay Detail
Binding
CHEMBL5738810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzymatic Assay: The IC50 values for aforementioned compounds against HDACs were determined. HDAC 1 to 11 can be assayed by using acetylated AMC-labeled peptide substrate. The Substrate 1, a fluorogenic peptide from p53 residues 379-382 (RHKKAc) is used for all MAC 1 to 11 but HDAC8, which has a substrate II (RHKAcKAc), a fluorogenic diacyl peptide based on residues 179-382 of p53. Compounds were tested in 10-dose 1050 mode in duplicate with 3-fold serial dilution starting at 10 uM.
81
Total Activities
26
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Histone deacetylases (HDACs) inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.39 | 9.00 |
| kon | 27 | - | - |
| k_off | 27 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | 1.0 | 6 | 9.00 |
| CHEMBL4550214 | — | — | 3 | 8.40 |
| CHEMBL5822037 | — | — | 3 | 8.40 |
| CHEMBL5396951 | — | — | 3 | 8.22 |
| CHEMBL4579683 | — | — | 3 | 8.10 |
| CHEMBL4442777 | — | — | 3 | 8.00 |
| CHEMBL5759520 | — | — | 3 | 7.96 |
| CHEMBL4554270 | — | — | 3 | 7.96 |
| CHEMBL5770781 | — | — | 3 | 7.85 |
| CHEMBL4457790 | — | — | 3 | 7.82 |
| CHEMBL4565933 | — | — | 3 | 7.68 |
| CHEMBL4453971 | — | — | 3 | 7.64 |
| CHEMBL5968609 | — | — | 3 | 7.62 |
| CHEMBL5891478 | — | — | 3 | 7.60 |
| CHEMBL4438057 | — | — | 3 | 7.55 |
| CHEMBL4441436 | — | — | 3 | 7.55 |
| CHEMBL4464975 | — | — | 3 | 7.46 |
| CHEMBL4537684 | — | — | 3 | 7.29 |
| CHEMBL4470654 | — | — | 3 | 7.24 |
| CHEMBL4474286 | — | — | 3 | 6.78 |
| CHEMBL4517827 | — | — | 3 | 6.77 |
| CHEMBL4513424 | — | — | 3 | 6.20 |
| CHEMBL4457073 | — | — | 3 | 5.92 |
| CHEMBL4473726 | — | — | 3 | 5.37 |
| CHEMBL5914638 | — | — | 3 | 5.35 |
| CHEMBL5436391 | — | — | 3 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL99 | TRICHOSTATIN | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4550214 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5822037 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5396951 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4579683 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4442777 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4554270 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5759520 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5770781 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4457790 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4565933 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4453971 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5968609 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5891478 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4438057 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4441436 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4464975 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4537684 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4470654 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4474286 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL4517827 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4513424 | — | IC50 | = | 635.0 | nM | 6.20 |
| CHEMBL4457073 | — | IC50 | = | 1194.0 | nM | 5.92 |
| CHEMBL4473726 | — | IC50 | = | 4296.0 | nM | 5.37 |
| CHEMBL5914638 | — | IC50 | = | 4450.0 | nM | 5.35 |
| CHEMBL5436391 | — | IC50 | = | 13500.0 | nM | 4.87 |
| CHEMBL4457790 | — | k_off | = | - | s-1 | - |
| CHEMBL4565933 | — | k_off | = | - | s-1 | - |
| CHEMBL4442777 | — | k_off | = | - | s-1 | - |
| CHEMBL4457073 | — | k_off | = | - | s-1 | - |
| CHEMBL4457073 | — | kon | = | - | — | - |
| CHEMBL4474286 | — | kon | = | - | — | - |
| CHEMBL5759520 | — | k_off | = | - | s-1 | - |
| CHEMBL5759520 | — | kon | = | - | — | - |
| CHEMBL4474286 | — | k_off | = | - | s-1 | - |
| CHEMBL4517827 | — | k_off | = | - | s-1 | - |
| CHEMBL5891478 | — | kon | = | - | — | - |
| CHEMBL4442777 | — | kon | = | - | — | - |
| CHEMBL4453971 | — | kon | = | - | — | - |
| CHEMBL4470654 | — | k_off | = | - | s-1 | - |
| CHEMBL99 | TRICHOSTATIN | k_off | = | - | s-1 | - |
| CHEMBL99 | TRICHOSTATIN | kon | = | - | — | - |
| CHEMBL5396951 | — | kon | = | - | — | - |
| CHEMBL4517827 | — | kon | = | - | — | - |
| CHEMBL5770781 | — | k_off | = | - | s-1 | - |
| CHEMBL5770781 | — | kon | = | - | — | - |
| CHEMBL5891478 | — | k_off | = | - | s-1 | - |
| CHEMBL4457790 | — | kon | = | - | — | - |
| CHEMBL5396951 | — | k_off | = | - | s-1 | - |