Assay Detail
Binding
CHEMBL4351618
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Binding affinity to human N-terminal His-tagged PCAF by isothermal titration calorimetry
34
Total Activities
34
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
Discovery of Pyrrolo[3,2- d]pyrimidin-4-one Derivatives as a New Class of Potent and Cell-Active Inhibitors of P300/CBP-Associated Factor Bromodomain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 6.34 | 7.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4574669 | — | — | 1 | 7.11 |
| CHEMBL4543497 | — | — | 1 | 7.07 |
| CHEMBL4453637 | — | — | 1 | 7.00 |
| CHEMBL4457684 | — | — | 1 | 6.99 |
| CHEMBL4454700 | — | — | 1 | 6.97 |
| CHEMBL4449143 | — | — | 1 | 6.93 |
| CHEMBL4570924 | — | — | 1 | 6.92 |
| CHEMBL4545594 | — | — | 1 | 6.89 |
| CHEMBL4527339 | — | — | 1 | 6.86 |
| CHEMBL4439202 | — | — | 1 | 6.85 |
| CHEMBL4471748 | — | — | 1 | 6.82 |
| CHEMBL4454766 | — | — | 1 | 6.74 |
| CHEMBL4565832 | — | — | 1 | 6.67 |
| CHEMBL4539318 | — | — | 1 | 6.63 |
| CHEMBL4541223 | — | — | 1 | 6.62 |
| CHEMBL4544739 | — | — | 1 | 6.46 |
| CHEMBL4525423 | — | — | 1 | 6.27 |
| CHEMBL4579627 | — | — | 1 | 6.21 |
| CHEMBL4453013 | — | — | 1 | 6.17 |
| CHEMBL4470046 | — | — | 1 | 6.09 |
| CHEMBL4547880 | — | — | 1 | 6.03 |
| CHEMBL4528565 | — | — | 1 | 5.92 |
| CHEMBL4438712 | — | — | 1 | 5.92 |
| CHEMBL4556786 | — | — | 1 | 5.67 |
| CHEMBL4449886 | — | — | 1 | 5.62 |
| CHEMBL4437954 | — | — | 1 | 5.52 |
| CHEMBL4537244 | — | — | 1 | 5.47 |
| CHEMBL4454395 | — | — | 1 | 5.11 |
| CHEMBL4475074 | — | — | 1 | 4.35 |
| CHEMBL4471746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4574669 | — | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL4543497 | — | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL4453637 | — | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL4457684 | — | Kd | = | 103.0 | nM | 6.99 |
| CHEMBL4454700 | — | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL4449143 | — | Kd | = | 118.0 | nM | 6.93 |
| CHEMBL4570924 | — | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL4545594 | — | Kd | = | 128.0 | nM | 6.89 |
| CHEMBL4527339 | — | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL4439202 | — | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL4471748 | — | Kd | = | 152.0 | nM | 6.82 |
| CHEMBL4454766 | — | Kd | = | 183.0 | nM | 6.74 |
| CHEMBL4565832 | — | Kd | = | 215.0 | nM | 6.67 |
| CHEMBL4539318 | — | Kd | = | 233.0 | nM | 6.63 |
| CHEMBL4541223 | — | Kd | = | 242.0 | nM | 6.62 |
| CHEMBL4544739 | — | Kd | = | 347.0 | nM | 6.46 |
| CHEMBL4525423 | — | Kd | = | 535.0 | nM | 6.27 |
| CHEMBL4579627 | — | Kd | = | 621.0 | nM | 6.21 |
| CHEMBL4453013 | — | Kd | = | 676.0 | nM | 6.17 |
| CHEMBL4470046 | — | Kd | = | 820.0 | nM | 6.09 |
| CHEMBL4547880 | — | Kd | = | 935.0 | nM | 6.03 |
| CHEMBL4528565 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL4438712 | — | Kd | = | 1190.0 | nM | 5.92 |
| CHEMBL4556786 | — | Kd | = | 2160.0 | nM | 5.67 |
| CHEMBL4449886 | — | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL4437954 | — | Kd | = | 3040.0 | nM | 5.52 |
| CHEMBL4537244 | — | Kd | = | 3410.0 | nM | 5.47 |
| CHEMBL4454395 | — | Kd | = | 7800.0 | nM | 5.11 |
| CHEMBL4475074 | — | Kd | = | 45000.0 | nM | 4.35 |
| CHEMBL4471746 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4471600 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4460616 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4581184 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL4584442 | — | Kd | > | 10000.0 | nM | - |