Assay Detail
Binding
CHEMBL5369311
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MCP-1 in LPS-stimulated human PBMC cells pretreated with compound for 30 mins followed by LPS-stimulation and measured after 10 mins by microplate analysis
16
Total Activities
16
Compounds Tested
2
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
Design and Characterization of 1,3-Dihydro-2<i>H</i>-benzo[<i>d</i>]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.11 | 10.40 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5426022 | — | — | 1 | 10.40 |
| CHEMBL5422047 | — | — | 1 | 9.60 |
| CHEMBL4078100 | AZD-5153 | 1.0 | 1 | 8.50 |
| CHEMBL1957266 | — | — | 1 | 8.20 |
| CHEMBL4438171 | — | — | 1 | 8.10 |
| CHEMBL4636881 | GSK046 | — | 1 | 7.50 |
| CHEMBL2017291 | — | — | 1 | 7.40 |
| CHEMBL4639128 | GSK778 | — | 1 | 7.40 |
| CHEMBL5220623 | — | — | 1 | 7.30 |
| CHEMBL4519518 | — | — | 1 | 6.70 |
| CHEMBL5426762 | — | — | 1 | - |
| CHEMBL5403564 | — | — | 1 | - |
| CHEMBL5408181 | — | — | 1 | - |
| CHEMBL5427202 | — | — | 1 | - |
| CHEMBL5417286 | — | — | 1 | - |
| CHEMBL5433432 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5426022 | — | IC50 | = | 0.03981 | nM | 10.40 |
| CHEMBL5422047 | — | IC50 | = | 0.2512 | nM | 9.60 |
| CHEMBL4078100 | AZD-5153 | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL1957266 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL4438171 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4636881 | GSK046 | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2017291 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL4639128 | GSK778 | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5220623 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL4519518 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5426762 | — | IC50 | < | 1.995 | nM | - |
| CHEMBL5403564 | — | IC50 | < | 1.995 | nM | - |
| CHEMBL5408181 | — | IC50 | < | 1.995 | nM | - |
| CHEMBL5427202 | — | pIC50 | - | — | - | |
| CHEMBL5417286 | — | pIC50 | - | — | - | |
| CHEMBL5433432 | — | IC50 | < | 0.1995 | nM | - |