Assay Detail
Binding
CHEMBL1074819
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Inhibition of human VLA4 in presence of 90% human plasma
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 9.56 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569263 | — | — | 1 | 9.96 |
| CHEMBL601687 | — | — | 1 | 9.96 |
| CHEMBL589749 | — | — | 1 | 9.89 |
| CHEMBL601686 | — | — | 1 | 9.89 |
| CHEMBL601688 | — | — | 1 | 9.89 |
| CHEMBL589558 | — | — | 1 | 9.85 |
| CHEMBL569255 | — | — | 1 | 9.80 |
| CHEMBL601896 | — | — | 1 | 9.80 |
| CHEMBL589750 | — | — | 1 | 9.80 |
| CHEMBL601685 | — | — | 1 | 9.60 |
| CHEMBL569403 | — | — | 1 | 9.47 |
| CHEMBL601684 | — | — | 1 | 9.38 |
| CHEMBL601467 | — | — | 1 | 9.32 |
| CHEMBL601683 | — | — | 1 | 9.30 |
| CHEMBL589748 | — | — | 1 | 8.70 |
| CHEMBL601682 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569263 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL601687 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL589749 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL601686 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL601688 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL589558 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL569255 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL601896 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL589750 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL601685 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL569403 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL601684 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL601467 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL601683 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL589748 | — | IC50 | = | 2.01 | nM | 8.70 |
| CHEMBL601682 | — | IC50 | = | 4.75 | nM | 8.32 |