Assay Detail
Binding
CHEMBL863348
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Displacement of [125I]-echistatin from alpha-v-beta-5 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 | 8.00 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL411941 | CYCLORGDFV | — | 1 | 9.96 |
| CHEMBL429876 | CILENGITIDE | 3.0 | 1 | 9.89 |
| CHEMBL556402 | — | — | 1 | 9.23 |
| CHEMBL392303 | — | — | 1 | 8.94 |
| CHEMBL534934 | — | — | 1 | 8.46 |
| CHEMBL557157 | — | — | 1 | 8.34 |
| CHEMBL540622 | — | — | 1 | 8.18 |
| CHEMBL534713 | — | — | 1 | 7.88 |
| CHEMBL534712 | — | — | 1 | 7.58 |
| CHEMBL534933 | — | — | 1 | 7.53 |
| CHEMBL534711 | — | — | 1 | 6.90 |
| CHEMBL539850 | — | — | 1 | 6.78 |
| CHEMBL539338 | — | — | 1 | 6.39 |
| CHEMBL540618 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL411941 | CYCLORGDFV | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL429876 | CILENGITIDE | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL556402 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL392303 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL534934 | — | IC50 | = | 3.43 | nM | 8.46 |
| CHEMBL557157 | — | IC50 | = | 4.56 | nM | 8.34 |
| CHEMBL540622 | — | IC50 | = | 6.56 | nM | 8.18 |
| CHEMBL534713 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL534712 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL534933 | — | IC50 | = | 29.6 | nM | 7.53 |
| CHEMBL534711 | — | IC50 | = | 125.4 | nM | 6.90 |
| CHEMBL539850 | — | IC50 | = | 165.5 | nM | 6.78 |
| CHEMBL539338 | — | IC50 | = | 411.5 | nM | 6.39 |
| CHEMBL540618 | — | IC50 | = | 1300.0 | nM | 5.89 |