Assay Detail
Binding
CHEMBL1043648
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Inhibition of VLA4 in human whole blood
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 9.33 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566154 | — | — | 1 | 10.15 |
| CHEMBL569442 | — | — | 1 | 8.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566154 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL569442 | — | IC50 | = | 3.1 | nM | 8.51 |