Assay Detail
Binding
CHEMBL5218150
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Inhibition of MCP-1 in LPS-stimulated human whole blood incubate for 24 hrs by immuno assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.66 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5220494 | — | — | 1 | 7.80 |
| CHEMBL5219991 | — | — | 1 | 7.70 |
| CHEMBL5218813 | — | — | 1 | 7.60 |
| CHEMBL5219919 | — | — | 1 | 7.50 |
| CHEMBL5220128 | — | — | 1 | 7.50 |
| CHEMBL5218909 | — | — | 1 | 7.40 |
| CHEMBL5218726 | — | — | 1 | 7.40 |
| CHEMBL5218822 | — | — | 1 | 7.40 |
| CHEMBL5219602 | — | — | 1 | 7.40 |
| CHEMBL5219538 | — | — | 1 | 7.40 |
| CHEMBL5221069 | — | — | 1 | 7.30 |
| CHEMBL5218817 | — | — | 1 | 7.30 |
| CHEMBL5219194 | — | — | 1 | 6.90 |
| CHEMBL5219077 | — | — | 1 | 6.80 |
| CHEMBL5220099 | — | — | 1 | 6.40 |
| CHEMBL5220077 | — | — | 1 | 6.40 |
| CHEMBL5220275 | — | — | 1 | 6.20 |
| CHEMBL5220753 | — | — | 1 | 6.20 |
| CHEMBL5220501 | — | — | 1 | 6.20 |
| CHEMBL5220904 | — | — | 1 | 6.20 |
| CHEMBL5219599 | — | — | 1 | 6.00 |
| CHEMBL5219089 | — | — | 1 | 6.00 |
| CHEMBL5218922 | — | — | 1 | 6.00 |
| CHEMBL5221107 | — | — | 1 | 5.90 |
| CHEMBL5220532 | — | — | 1 | 5.80 |
| CHEMBL5220993 | — | — | 1 | 5.80 |
| CHEMBL5218619 | — | — | 1 | 5.70 |
| CHEMBL5218824 | — | — | 1 | 5.50 |
| CHEMBL5221111 | — | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5220494 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL5219991 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL5218813 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL5219919 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5220128 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL5218909 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5218726 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5218822 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5219602 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5219538 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL5221069 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5218817 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5219194 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL5219077 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL5220099 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5220077 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL5220275 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5220753 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5220501 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5220904 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5219599 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5219089 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5218922 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5221107 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL5220532 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL5220993 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL5218619 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL5218824 | — | IC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL5221111 | — | IC50 | = | 5011.87 | nM | 5.30 |