Assay Detail
Binding
CHEMBL4053008
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Inhibition of human BRPF2-BRD1 expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay
11
Total Activities
11
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
Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.34 | 7.32 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102050 | — | — | 1 | 7.32 |
| CHEMBL4069814 | — | — | 1 | 6.89 |
| CHEMBL4076056 | — | — | 1 | 6.70 |
| CHEMBL4099455 | — | — | 1 | 6.64 |
| CHEMBL4103432 | — | — | 1 | 6.57 |
| CHEMBL4081438 | — | — | 1 | 6.35 |
| CHEMBL4067436 | — | — | 1 | 5.85 |
| CHEMBL4070377 | — | — | 1 | 5.77 |
| CHEMBL4096095 | — | — | 1 | 5.75 |
| CHEMBL4078047 | — | — | 1 | 5.58 |
| CHEMBL4059509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102050 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4069814 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4076056 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4099455 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4103432 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4081438 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4067436 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4070377 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4096095 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4078047 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4059509 | — | IC50 | > | 100000.0 | nM | - |