Assay Detail
Binding
CHEMBL4194907
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Binding affinity to BRD4 bromodomain 2 (E352 to M457 amino acids) (unknown origin) using Alexa647-labeled BET-inhibitor as fluorescent probe by bromodomain TR-FRET binding assay
3
Total Activities
3
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
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.85 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217457 | — | — | 1 | 9.14 |
| CHEMBL4208129 | — | — | 1 | 8.82 |
| CHEMBL4215988 | — | — | 1 | 8.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217457 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL4208129 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL4215988 | — | Ki | = | 2.5 | nM | 8.60 |