Assay Detail
Binding
CHEMBL5163975
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HDAC1 (unknown origin) using trypsin and LGK(Ac)-AMC as substrates incubated for 1 hr and measured by fluorescence assay
44
Total Activities
44
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
Dual-acting antitumor agents targeting the A<sub>2A</sub> adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.26 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5169828 | — | — | 1 | 8.66 |
| CHEMBL5197839 | — | — | 1 | 8.62 |
| CHEMBL5185100 | — | — | 1 | 8.15 |
| CHEMBL5202905 | — | — | 1 | 8.14 |
| CHEMBL5205993 | — | — | 1 | 8.14 |
| CHEMBL5208818 | — | — | 1 | 8.08 |
| CHEMBL5207324 | — | — | 1 | 8.03 |
| CHEMBL5169338 | — | — | 1 | 8.03 |
| CHEMBL5190098 | — | — | 1 | 7.96 |
| CHEMBL5209296 | — | — | 1 | 7.89 |
| CHEMBL5170997 | — | — | 1 | 7.85 |
| CHEMBL5190589 | — | — | 1 | 7.84 |
| CHEMBL5184684 | — | — | 1 | 7.76 |
| CHEMBL5201523 | — | — | 1 | 7.73 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 7.68 |
| CHEMBL5188801 | — | — | 1 | 7.64 |
| CHEMBL5171672 | — | — | 1 | 7.53 |
| CHEMBL5195323 | — | — | 1 | 7.43 |
| CHEMBL5179765 | — | — | 1 | 7.37 |
| CHEMBL5204735 | — | — | 1 | 7.35 |
| CHEMBL5171122 | — | — | 1 | 7.35 |
| CHEMBL5201509 | — | — | 1 | 7.19 |
| CHEMBL5200340 | — | — | 1 | 7.13 |
| CHEMBL5189051 | — | — | 1 | 7.07 |
| CHEMBL272980 | MOCETINOSTAT | 2.0 | 1 | 7.06 |
| CHEMBL5186576 | — | — | 1 | 7.02 |
| CHEMBL5203443 | — | — | 1 | 6.98 |
| CHEMBL5207247 | — | — | 1 | 6.93 |
| CHEMBL5176483 | — | — | 1 | 6.90 |
| CHEMBL5193403 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5169828 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL5197839 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5185100 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL5202905 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5205993 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5208818 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5207324 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5169338 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL5190098 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL5209296 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL5170997 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5190589 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5184684 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL5201523 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL98 | VORINOSTAT | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5188801 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5171672 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL5195323 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5179765 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL5204735 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5171122 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5201509 | — | IC50 | = | 64.5 | nM | 7.19 |
| CHEMBL5200340 | — | IC50 | = | 73.5 | nM | 7.13 |
| CHEMBL5189051 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL272980 | MOCETINOSTAT | IC50 | = | 86.3 | nM | 7.06 |
| CHEMBL5186576 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5203443 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5207247 | — | IC50 | = | 116.5 | nM | 6.93 |
| CHEMBL5176483 | — | IC50 | = | 126.3 | nM | 6.90 |
| CHEMBL5193403 | — | IC50 | = | 126.5 | nM | 6.90 |
| CHEMBL5199428 | — | IC50 | = | 145.3 | nM | 6.84 |
| CHEMBL5171906 | — | IC50 | = | 151.0 | nM | 6.82 |
| CHEMBL5202005 | — | IC50 | = | 185.5 | nM | 6.73 |
| CHEMBL5205560 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5188108 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL5196802 | — | IC50 | = | 205.5 | nM | 6.69 |
| CHEMBL5189321 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5190722 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL5192939 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL5194109 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL5200632 | — | IC50 | = | 419.5 | nM | 6.38 |
| CHEMBL5179716 | — | IC50 | = | 573.5 | nM | 6.24 |
| CHEMBL5173073 | — | IC50 | = | 1175.5 | nM | 5.93 |
| CHEMBL5194232 | — | IC50 | = | 2532.0 | nM | 5.60 |