Assay Detail
Binding
CHEMBL3382827
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of biotinylated tetra-acetylated histone H4 from His6-tagged BRD2 (1 to 473 aa) (unknown origin) after 1 hr by TR-FRET assay
31
Total Activities
29
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
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 5.89 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2177300 | — | — | 2 | 6.80 |
| CHEMBL3353999 | — | — | 2 | 6.70 |
| CHEMBL3353992 | — | — | 1 | 6.30 |
| CHEMBL3353996 | — | — | 1 | 6.30 |
| CHEMBL3352833 | — | — | 1 | 6.20 |
| CHEMBL3354004 | — | — | 1 | 6.20 |
| CHEMBL3354003 | — | — | 1 | 6.20 |
| CHEMBL3354008 | — | — | 1 | 6.10 |
| CHEMBL3353984 | — | — | 1 | 6.10 |
| CHEMBL3354006 | — | — | 1 | 6.10 |
| CHEMBL3353989 | — | — | 1 | 6.10 |
| CHEMBL3353990 | — | — | 1 | 6.10 |
| CHEMBL3353997 | — | — | 1 | 6.00 |
| CHEMBL3354005 | — | — | 1 | 6.00 |
| CHEMBL3353985 | — | — | 1 | 6.00 |
| CHEMBL3353998 | — | — | 1 | 5.90 |
| CHEMBL3354001 | — | — | 1 | 5.90 |
| CHEMBL3353991 | — | — | 1 | 5.90 |
| CHEMBL3353988 | — | — | 1 | 5.90 |
| CHEMBL3353986 | — | — | 1 | 5.90 |
| CHEMBL3354000 | — | — | 1 | 5.80 |
| CHEMBL3354002 | — | — | 1 | 5.80 |
| CHEMBL3353987 | — | — | 1 | 5.70 |
| CHEMBL3354007 | — | — | 1 | 5.70 |
| CHEMBL3354009 | — | — | 1 | 5.40 |
| CHEMBL3354010 | — | — | 1 | 5.20 |
| CHEMBL3353993 | — | — | 1 | 4.80 |
| CHEMBL3353995 | — | — | 1 | 4.60 |
| CHEMBL3353994 | — | — | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2177300 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3353999 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL2177300 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL3353992 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3353996 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3353999 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3352833 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3354004 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3354003 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL3353984 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3354008 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3353989 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3353990 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3354006 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3354005 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3353997 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3353985 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3353998 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3354001 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3353991 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3353988 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3353986 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL3354000 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3354002 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3354007 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3353987 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL3354009 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL3354010 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL3353993 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL3353995 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL3353994 | — | IC50 | = | 50118.72 | nM | 4.30 |