Assay Detail
Binding
CHEMBL1006963
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Inhibition of GST-fused recombinant HAT PCAF expressed in Escherichia coli by filter assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 4.96 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL499919 | — | — | 1 | 5.82 |
| CHEMBL489101 | — | — | 1 | 5.51 |
| CHEMBL489102 | — | — | 1 | 5.27 |
| CHEMBL443951 | — | — | 1 | 5.27 |
| CHEMBL316658 | — | — | 1 | 5.21 |
| CHEMBL487498 | — | — | 1 | 5.19 |
| CHEMBL491092 | — | — | 1 | 5.12 |
| CHEMBL489494 | — | — | 1 | 4.72 |
| CHEMBL501034 | — | — | 1 | 4.70 |
| CHEMBL99594 | — | — | 1 | 4.55 |
| CHEMBL474276 | — | — | 1 | 4.50 |
| CHEMBL487269 | — | — | 1 | 4.37 |
| CHEMBL489495 | — | — | 1 | 4.24 |
| CHEMBL521918 | — | — | 1 | - |
| CHEMBL489895 | — | — | 1 | - |
| CHEMBL500224 | — | — | 1 | - |
| CHEMBL489896 | — | — | 1 | - |
| CHEMBL490884 | — | — | 1 | - |
| CHEMBL491476 | — | — | 1 | - |
| CHEMBL445189 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL499919 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL489101 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL489102 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL443951 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL316658 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL487498 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL491092 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL489494 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL501034 | — | IC50 | = | 19800.0 | nM | 4.70 |
| CHEMBL99594 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL474276 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL487269 | — | IC50 | = | 42700.0 | nM | 4.37 |
| CHEMBL489495 | — | IC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL521918 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL489895 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL500224 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL489896 | — | IC50 | = | 102000.0 | nM | - |
| CHEMBL490884 | — | IC50 | > | 200000.0 | nM | - |
| CHEMBL491476 | — | IC50 | = | 162000.0 | nM | - |
| CHEMBL445189 | — | IC50 | = | 109000.0 | nM | - |