Assay Detail
Binding
CHEMBL4051532
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human BRPF2 (563 to 688 residues) expressed in Escherichia coli BL21 (DE3)-R3-pRARE2 preincubated for 15 mins followed by addition of C-terminal biotinylated synthetic K5,12 diacetylated histone H4 (1 to 20 residues) peptide as substrate measured after 1 hr by TR-FRET assay
29
Total Activities
27
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
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.99 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4075478 | — | — | 1 | 7.43 |
| CHEMBL4086958 | — | — | 1 | 7.29 |
| CHEMBL4104538 | — | — | 1 | 7.28 |
| CHEMBL4086276 | — | — | 3 | 7.21 |
| CHEMBL4067968 | — | — | 1 | 7.21 |
| CHEMBL4076603 | — | — | 1 | 7.20 |
| CHEMBL4065133 | — | — | 1 | 7.18 |
| CHEMBL4059651 | — | — | 1 | 7.16 |
| CHEMBL4064164 | — | — | 1 | 7.13 |
| CHEMBL4076067 | — | — | 1 | 7.10 |
| CHEMBL4068180 | — | — | 1 | 7.09 |
| CHEMBL4091912 | — | — | 1 | 7.08 |
| CHEMBL4098824 | — | — | 1 | 7.03 |
| CHEMBL4072812 | — | — | 1 | 7.03 |
| CHEMBL4092917 | — | — | 1 | 7.02 |
| CHEMBL4064292 | — | — | 1 | 7.00 |
| CHEMBL4077317 | — | — | 1 | 6.99 |
| CHEMBL4080780 | — | — | 1 | 6.94 |
| CHEMBL4062266 | — | — | 1 | 6.92 |
| CHEMBL4081145 | — | — | 1 | 6.91 |
| CHEMBL4063112 | — | — | 1 | 6.90 |
| CHEMBL4075962 | — | — | 1 | 6.82 |
| CHEMBL4099171 | — | — | 1 | 6.61 |
| CHEMBL4064184 | — | — | 1 | 6.44 |
| CHEMBL4077619 | — | — | 1 | 6.35 |
| CHEMBL3356143 | — | — | 1 | 5.96 |
| CHEMBL4067538 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4075478 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4086958 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4104538 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4086276 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4067968 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4076603 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4065133 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4086276 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4059651 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4064164 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4086276 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4076067 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4068180 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4091912 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4072812 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4098824 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4092917 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4064292 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4077317 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4080780 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4062266 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4081145 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL4063112 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4075962 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4099171 | — | IC50 | = | 248.0 | nM | 6.61 |
| CHEMBL4064184 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL4077619 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3356143 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL4067538 | — | IC50 | > | 20000.0 | nM | - |