Assay Detail
Binding
CHEMBL4003557
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Halo-tagged histone H3.3 from NanoLuc-tagged full length human PCAF bromodomain expressed in HEK293 cells after 18 hrs by NanoBRET assay
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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 | 4 | 6.11 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4069412 | — | — | 2 | 7.22 |
| CHEMBL4096641 | — | — | 2 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4069412 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4069412 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4096641 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4096641 | — | IC50 | = | 10000.0 | nM | 5.00 |