Assay Detail
Binding
CHEMBL4051111
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 in human NCI-H1299 cells after 24 hrs by Bright-Glo luciferase reporter gene assay
39
Total Activities
39
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
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 39 | 6.98 | 8.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073279 | — | — | 1 | 8.29 |
| CHEMBL4068431 | — | — | 1 | 8.19 |
| CHEMBL4099010 | — | — | 1 | 8.19 |
| CHEMBL4090068 | — | — | 1 | 8.17 |
| CHEMBL4075776 | — | — | 1 | 8.03 |
| CHEMBL4075567 | — | — | 1 | 7.80 |
| CHEMBL4089651 | — | — | 1 | 7.75 |
| CHEMBL4077124 | — | — | 1 | 7.62 |
| CHEMBL4068991 | — | — | 1 | 7.58 |
| CHEMBL4091597 | — | — | 1 | 7.57 |
| CHEMBL4075757 | — | — | 1 | 7.47 |
| CHEMBL4094644 | — | — | 1 | 7.46 |
| CHEMBL4078875 | — | — | 1 | 7.41 |
| CHEMBL4082889 | — | — | 1 | 7.41 |
| CHEMBL4059680 | — | — | 1 | 7.35 |
| CHEMBL4083186 | — | — | 1 | 7.32 |
| CHEMBL4101823 | — | — | 1 | 7.26 |
| CHEMBL4099335 | — | — | 1 | 7.25 |
| CHEMBL4071697 | — | — | 1 | 7.18 |
| CHEMBL4103153 | — | — | 1 | 7.17 |
| CHEMBL4063808 | — | — | 1 | 7.16 |
| CHEMBL4091093 | — | — | 1 | 7.11 |
| CHEMBL4078459 | — | — | 1 | 7.00 |
| CHEMBL4093439 | — | — | 1 | 6.85 |
| CHEMBL4061006 | — | — | 1 | 6.82 |
| CHEMBL4102713 | — | — | 1 | 6.75 |
| CHEMBL4083819 | — | — | 1 | 6.68 |
| CHEMBL4090979 | — | — | 1 | 6.64 |
| CHEMBL4072862 | — | — | 1 | 6.64 |
| CHEMBL4099746 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073279 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4068431 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4099010 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4090068 | — | EC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4075776 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL4075567 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4089651 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4077124 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4068991 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4091597 | — | EC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4075757 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4094644 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4078875 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4082889 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4059680 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4083186 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4101823 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4099335 | — | EC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4071697 | — | EC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4103153 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4063808 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4091093 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4078459 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4093439 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4061006 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4102713 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4083819 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4090979 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4072862 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4099746 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4072399 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4063083 | — | EC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4101187 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4072714 | — | EC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4070131 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4083304 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL4064267 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4092002 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4061472 | — | EC50 | = | 4900.0 | nM | 5.31 |