Assay Detail
Binding
CHEMBL4650004
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Alphascreen assay. Binding to BRD4A (domain start/stop: N44-E168) by alphascreen assay
8
Total Activities
5
Compounds Tested
1
Activity Types
3
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Category | Alphascreen assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
EUbOPEN bromodomain assay panel
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.97 | 7.59 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Protein Sequence | Protein Sequence | - | — | MHHHHHHSSGVDLGTENLYFQSMNPPPPETSNPNKPKRQTNQLQYLLRVVLKTLWKHQFAWPFQQPVDAVKLNLPDYYKIIKTPMDMGTIKKRLENNYYWNAQECIQDFNTMFTNCYIYNKPGDDIVLMAEALEKLFLQKINELPTEE |
| Refseq Start/Stop | Refseq Start/Stop | - | — | N44-E168 |
| Target UniProt Accession | Target UniProt Accession | - | — | O60885 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2132936 | — | — | 1 | 7.59 |
| CHEMBL3133807 | — | — | 3 | 7.08 |
| CHEMBL3774655 | — | — | 1 | 5.61 |
| CHEMBL3622373 | — | — | 2 | 5.15 |
| CHEMBL3769507 | — | — | 1 | 4.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2132936 | — | IC50 | = | 25.4 | nM | 7.59 |
| CHEMBL3133807 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3133807 | — | IC50 | = | 310.9 | nM | 6.51 |
| CHEMBL3133807 | — | IC50 | = | 468.4 | nM | 6.33 |
| CHEMBL3774655 | — | IC50 | = | 2456.1 | nM | 5.61 |
| CHEMBL3622373 | — | IC50 | = | 7121.2 | nM | 5.15 |
| CHEMBL3769507 | — | IC50 | = | 11190.0 | nM | 4.95 |
| CHEMBL3622373 | — | IC50 | = | 27790.0 | nM | 4.56 |