Assay Detail
Binding
CHEMBL4038392
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Binding affinity to His-tagged BRD4 BD1-BD2 (K57 to K550 residues) (unknown origin) after 1 hr by Alexa-647-conjugated probe based TR-FRET assay
40
Total Activities
40
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
Methylpyrrole inhibitors of BET bromodomains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 6.68 | 8.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4064089 | — | — | 1 | 8.26 |
| CHEMBL4064625 | — | — | 1 | 8.00 |
| CHEMBL4097720 | — | — | 1 | 7.96 |
| CHEMBL4096183 | — | — | 1 | 7.96 |
| CHEMBL4074813 | — | — | 1 | 7.80 |
| CHEMBL3769755 | — | — | 1 | 7.77 |
| CHEMBL4068902 | — | — | 1 | 7.77 |
| CHEMBL4079684 | — | — | 1 | 7.77 |
| CHEMBL4086135 | — | — | 1 | 7.52 |
| CHEMBL4063051 | — | — | 1 | 7.48 |
| CHEMBL4102516 | — | — | 1 | 7.43 |
| CHEMBL4087079 | — | — | 1 | 7.39 |
| CHEMBL4095264 | — | — | 1 | 7.11 |
| CHEMBL4067320 | — | — | 1 | 7.08 |
| CHEMBL4080666 | — | — | 1 | 7.04 |
| CHEMBL4088466 | — | — | 1 | 7.01 |
| CHEMBL4097227 | — | — | 1 | 7.01 |
| CHEMBL4103937 | — | — | 1 | 6.92 |
| CHEMBL4080682 | — | — | 1 | 6.82 |
| CHEMBL4069994 | — | — | 1 | 6.68 |
| CHEMBL4098709 | — | — | 1 | 6.60 |
| CHEMBL4065327 | — | — | 1 | 6.57 |
| CHEMBL4060309 | — | — | 1 | 6.55 |
| CHEMBL3786012 | — | — | 1 | 6.52 |
| CHEMBL4104934 | — | — | 1 | 6.47 |
| CHEMBL4074891 | — | — | 1 | 6.43 |
| CHEMBL4098863 | — | — | 1 | 6.39 |
| CHEMBL4088536 | — | — | 1 | 6.38 |
| CHEMBL4068988 | — | — | 1 | 6.36 |
| CHEMBL4078245 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4064089 | — | Ki | = | 5.5 | nM | 8.26 |
| CHEMBL4064625 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4096183 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4097720 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4074813 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3769755 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4068902 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4079684 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4086135 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4063051 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4102516 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4087079 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4095264 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4067320 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL4080666 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL4088466 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4097227 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL4103937 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL4080682 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4069994 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4098709 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL4065327 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL4060309 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL3786012 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL4104934 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4074891 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL4098863 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL4088536 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL4068988 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL4086753 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4078245 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4079208 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL4076251 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL4080820 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL4095330 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL4096256 | — | Ki | = | 9500.0 | nM | 5.02 |
| CHEMBL4068905 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL4079686 | — | Ki | = | 21000.0 | nM | 4.68 |
| CHEMBL4073935 | — | Ki | = | 22000.0 | nM | 4.66 |
| CHEMBL4089989 | — | Ki | = | 25000.0 | nM | 4.60 |