Assay Detail
Binding
CHEMBL4003553
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of GSK3103956A from human BRD4 (1 to 477 residues) BD1 Y390A mutant incubated for 30 mins in dark by TR-FRET assay
21
Total Activities
21
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 a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 4.68 | 4.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085471 | — | — | 1 | 4.80 |
| CHEMBL4096572 | — | — | 1 | 4.80 |
| CHEMBL4074202 | — | — | 1 | 4.70 |
| CHEMBL4095646 | — | — | 1 | 4.70 |
| CHEMBL4075248 | — | — | 1 | 4.60 |
| CHEMBL4065579 | — | — | 1 | 4.50 |
| CHEMBL4063947 | — | — | 1 | - |
| CHEMBL4091717 | — | — | 1 | - |
| CHEMBL4101945 | — | — | 1 | - |
| CHEMBL4101756 | — | — | 1 | - |
| CHEMBL4071581 | — | — | 1 | - |
| CHEMBL4093233 | — | — | 1 | - |
| CHEMBL4100959 | — | — | 1 | - |
| CHEMBL4096641 | — | — | 1 | - |
| CHEMBL4069412 | — | — | 1 | - |
| CHEMBL4061691 | — | — | 1 | - |
| CHEMBL4084253 | — | — | 1 | - |
| CHEMBL4083019 | — | — | 1 | - |
| CHEMBL4061142 | — | — | 1 | - |
| CHEMBL4099456 | — | — | 1 | - |
| CHEMBL4072538 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085471 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4096572 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4074202 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4095646 | — | IC50 | = | 19952.62 | nM | 4.70 |
| CHEMBL4075248 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4065579 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4063947 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4091717 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4101945 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4101756 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4071581 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4093233 | — | IC50 | = | 125892.54 | nM | - |
| CHEMBL4100959 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4096641 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4069412 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4061691 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4084253 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4083019 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4061142 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4099456 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4072538 | — | IC50 | > | 50118.72 | nM | - |