Assay Detail
Binding
CHEMBL863347
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Displacement of [125I]-echistatin from alphavbeta3 integrin receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.72 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL392303 | — | — | 1 | 8.85 |
| CHEMBL556402 | — | — | 1 | 8.82 |
| CHEMBL534934 | — | — | 1 | 8.34 |
| CHEMBL557157 | — | — | 1 | 8.25 |
| CHEMBL534713 | — | — | 1 | 8.14 |
| CHEMBL540622 | — | — | 1 | 8.11 |
| CHEMBL534712 | — | — | 1 | 8.00 |
| CHEMBL429876 | CILENGITIDE | 3.0 | 1 | 7.72 |
| CHEMBL534933 | — | — | 1 | 7.45 |
| CHEMBL534711 | — | — | 1 | 7.35 |
| CHEMBL539850 | — | — | 1 | 7.29 |
| CHEMBL539338 | — | — | 1 | 6.88 |
| CHEMBL411941 | CYCLORGDFV | — | 1 | 6.71 |
| CHEMBL540618 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL392303 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL556402 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL534934 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL557157 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL534713 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL540622 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL534712 | — | IC50 | = | 9.93 | nM | 8.00 |
| CHEMBL429876 | CILENGITIDE | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL534933 | — | IC50 | = | 35.6 | nM | 7.45 |
| CHEMBL534711 | — | IC50 | = | 44.7 | nM | 7.35 |
| CHEMBL539850 | — | IC50 | = | 51.4 | nM | 7.29 |
| CHEMBL539338 | — | IC50 | = | 132.9 | nM | 6.88 |
| CHEMBL411941 | CYCLORGDFV | IC50 | = | 195.9 | nM | 6.71 |
| CHEMBL540618 | — | IC50 | = | 712.7 | nM | 6.15 |