Assay Detail
Binding
CHEMBL4404018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Alexa Fluor 647 labelled ligand from recombinant human N-terminal His6-tagged BRD4 BD1 (1 to 477 residues)/BD2 Y390A mutant incubated for 30 mins by TR-FRET assay
31
Total Activities
27
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.47 | 8.00 |
| pIC50 | 1 | - | - |
| Kd | 1 | 8.30 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4438171 | — | — | 2 | 8.30 |
| CHEMBL4448056 | — | — | 1 | 8.00 |
| CHEMBL4522991 | — | — | 2 | 7.60 |
| CHEMBL4576013 | — | — | 1 | 7.40 |
| CHEMBL4579229 | — | — | 1 | 7.30 |
| CHEMBL4547614 | — | — | 1 | 7.30 |
| CHEMBL4466159 | — | — | 2 | 7.20 |
| CHEMBL4570497 | — | — | 1 | 7.10 |
| CHEMBL4456922 | — | — | 1 | 7.10 |
| CHEMBL4459169 | — | — | 2 | 6.80 |
| CHEMBL4457453 | — | — | 1 | 6.70 |
| CHEMBL4455610 | — | — | 1 | 6.60 |
| CHEMBL4475163 | — | — | 1 | 6.50 |
| CHEMBL4581846 | — | — | 1 | 6.30 |
| CHEMBL4460392 | — | — | 1 | 6.30 |
| CHEMBL4469520 | — | — | 1 | 6.20 |
| CHEMBL4466558 | — | — | 1 | 5.80 |
| CHEMBL4439664 | — | — | 1 | 5.80 |
| CHEMBL4443443 | — | — | 1 | 5.80 |
| CHEMBL4572090 | — | — | 1 | 5.80 |
| CHEMBL4464453 | — | — | 1 | 5.70 |
| CHEMBL4574340 | — | — | 1 | 5.60 |
| CHEMBL4450089 | — | — | 1 | 5.20 |
| CHEMBL4553071 | — | — | 1 | 5.10 |
| CHEMBL4452292 | — | — | 1 | 4.90 |
| CHEMBL4558654 | — | — | 1 | - |
| CHEMBL4593025 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4438171 | — | Kd | = | 5.012 | nM | 8.30 |
| CHEMBL4448056 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4438171 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL4522991 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4522991 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL4576013 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4579229 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4547614 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4466159 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4570497 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4456922 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL4459169 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4457453 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4455610 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4475163 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4460392 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4581846 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4469520 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4459169 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4466558 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4439664 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4572090 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4443443 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4464453 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4574340 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4466159 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4450089 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4553071 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4452292 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4558654 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4593025 | — | pIC50 | - | — | - |