Assay Detail
Binding
CHEMBL4843799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 in human whole blood assessed as reduction in LPS-induced IL-6 secretion preincubated for 30 mins followed by LPS stimulation and measured after 24 hrs by MSD assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.39 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874801 | — | — | 1 | 6.80 |
| CHEMBL4853472 | — | — | 1 | 6.70 |
| CHEMBL4874356 | — | — | 1 | 6.60 |
| CHEMBL4861790 | — | — | 1 | 6.60 |
| CHEMBL4878439 | — | — | 1 | 6.50 |
| CHEMBL4875886 | — | — | 1 | 6.50 |
| CHEMBL4874790 | — | — | 1 | 6.40 |
| CHEMBL4855373 | — | — | 1 | 6.40 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 6.20 |
| CHEMBL2017291 | — | — | 1 | 5.90 |
| CHEMBL4849704 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4874801 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4853472 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4874356 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4861790 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4878439 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4875886 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4874790 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4855373 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2017291 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4849704 | — | IC50 | = | 1995.26 | nM | 5.70 |