Assay Detail
Binding
CHEMBL4053000
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Inhibition of human BRPF1 expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay
16
Total Activities
16
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 | 16 | 7.00 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4102050 | — | — | 1 | 8.10 |
| CHEMBL4069814 | — | — | 1 | 8.05 |
| CHEMBL4097011 | — | — | 1 | 7.82 |
| CHEMBL4076056 | — | — | 1 | 7.37 |
| CHEMBL4099455 | — | — | 1 | 7.36 |
| CHEMBL4103432 | — | — | 1 | 7.25 |
| CHEMBL4096095 | — | — | 1 | 7.22 |
| CHEMBL4081438 | — | — | 1 | 7.21 |
| CHEMBL4067436 | — | — | 1 | 7.19 |
| CHEMBL4080511 | — | — | 1 | 6.75 |
| CHEMBL4079041 | — | — | 1 | 6.72 |
| CHEMBL4078047 | — | — | 1 | 6.66 |
| CHEMBL4070377 | — | — | 1 | 6.37 |
| CHEMBL4095549 | — | — | 1 | 5.68 |
| CHEMBL216146 | — | — | 1 | 5.32 |
| CHEMBL4059509 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4102050 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4069814 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4097011 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4076056 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4099455 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4103432 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4096095 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4081438 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4067436 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4080511 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4079041 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4078047 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4070377 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4095549 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL216146 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4059509 | — | IC50 | > | 100000.0 | nM | - |