Assay Detail
Binding
CHEMBL818376
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Inhibition of [125I]VCAM-Ig binding to alpha4-beta7 integrin of human RPMI-8866 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | RPMI-8866 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.66 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL56511 | — | — | 1 | 8.53 |
| CHEMBL88608 | — | — | 1 | 7.88 |
| CHEMBL90637 | — | — | 1 | 7.61 |
| CHEMBL91109 | — | — | 1 | 7.11 |
| CHEMBL90580 | — | — | 1 | 7.08 |
| CHEMBL330340 | — | — | 1 | 6.62 |
| CHEMBL94107 | — | — | 1 | 6.51 |
| CHEMBL93790 | — | — | 1 | 6.46 |
| CHEMBL328973 | — | — | 1 | 6.38 |
| CHEMBL88478 | — | — | 1 | 6.36 |
| CHEMBL92200 | — | — | 1 | 5.94 |
| CHEMBL91136 | — | — | 1 | 5.91 |
| CHEMBL90995 | — | — | 1 | 5.65 |
| CHEMBL91030 | — | — | 1 | 5.24 |
| CHEMBL93700 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL56511 | — | IC50 | = | 2.98 | nM | 8.53 |
| CHEMBL88608 | — | IC50 | = | 13.2 | nM | 7.88 |
| CHEMBL90637 | — | IC50 | = | 24.32 | nM | 7.61 |
| CHEMBL91109 | — | IC50 | = | 78.25 | nM | 7.11 |
| CHEMBL90580 | — | IC50 | = | 82.7 | nM | 7.08 |
| CHEMBL330340 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL94107 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL93790 | — | IC50 | = | 344.5 | nM | 6.46 |
| CHEMBL328973 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL88478 | — | IC50 | = | 433.0 | nM | 6.36 |
| CHEMBL92200 | — | IC50 | = | 1140.8 | nM | 5.94 |
| CHEMBL91136 | — | IC50 | = | 1235.0 | nM | 5.91 |
| CHEMBL90995 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL91030 | — | IC50 | = | 5720.0 | nM | 5.24 |
| CHEMBL93700 | — | IC50 | > | 4000.0 | nM | - |