Assay Detail
Binding
CHEMBL4843798
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BRD4 in human PBMC assessed as reduction in LPS-induced IL-6 secretion incubated for 18 to 24 hrs by MSD assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| 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 | 34 | 6.48 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4861790 | — | — | 1 | 7.60 |
| CHEMBL4874801 | — | — | 1 | 7.60 |
| CHEMBL4874356 | — | — | 1 | 7.40 |
| CHEMBL4862592 | — | — | 1 | 7.40 |
| CHEMBL4853472 | — | — | 1 | 7.00 |
| CHEMBL4878439 | — | — | 1 | 7.00 |
| CHEMBL4874790 | — | — | 1 | 7.00 |
| CHEMBL4864056 | — | — | 1 | 6.90 |
| CHEMBL4855373 | — | — | 1 | 6.90 |
| CHEMBL4874457 | — | — | 1 | 6.90 |
| CHEMBL4862999 | — | — | 1 | 6.80 |
| CHEMBL4847186 | — | — | 1 | 6.80 |
| CHEMBL4846393 | — | — | 1 | 6.80 |
| CHEMBL4869970 | — | — | 1 | 6.70 |
| CHEMBL4859880 | — | — | 1 | 6.70 |
| CHEMBL2017291 | — | — | 1 | 6.70 |
| CHEMBL4855128 | — | — | 1 | 6.60 |
| CHEMBL1232461 | MOLIBRESIB | 2.0 | 1 | 6.50 |
| CHEMBL4849704 | — | — | 1 | 6.50 |
| CHEMBL4861057 | — | — | 1 | 6.40 |
| CHEMBL4846391 | — | — | 1 | 6.40 |
| CHEMBL4875479 | — | — | 1 | 6.40 |
| CHEMBL2017286 | — | — | 1 | 6.30 |
| CHEMBL4875886 | — | — | 1 | 6.30 |
| CHEMBL4862100 | — | — | 1 | 6.20 |
| CHEMBL4859354 | — | — | 1 | 6.00 |
| CHEMBL4877490 | — | — | 1 | 5.90 |
| CHEMBL4861475 | — | — | 1 | 5.80 |
| CHEMBL4873648 | — | — | 1 | 5.80 |
| CHEMBL4871914 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4861790 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4874801 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL4874356 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4862592 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4853472 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4878439 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4874790 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4864056 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4855373 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4874457 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL4862999 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4847186 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL4846393 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL2017291 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4859880 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4869970 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL4855128 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL1232461 | MOLIBRESIB | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4849704 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4861057 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4846391 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL4875479 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL2017286 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4875886 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL4862100 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL4859354 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4877490 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4861475 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4873648 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4871914 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL4859578 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4869121 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL4861667 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL4864900 | — | IC50 | = | 15848.93 | nM | 4.80 |