Assay Detail
Binding
CHEMBL3877181
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Inhibition of N-terminal 6His-tagged human BRD4 bromodomain 1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) using biotinylated histone H4 peptide (1 to 21 residues) containing KAc (K5/8/12/16Ac) as substrate by Alpha screen assay
6
Total Activities
6
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
Non-kinase targets of protein kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.54 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 7.60 |
| CHEMBL2132936 | — | — | 1 | 7.46 |
| CHEMBL1995703 | — | — | 1 | 6.89 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.54 |
| CHEMBL188678 | — | — | 1 | 6.00 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513909 | BI-2536 | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2132936 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1995703 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1287853 | FEDRATINIB | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL188678 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2103840 | DINACICLIB | IC50 | = | 19000.0 | nM | 4.72 |