Assay Detail
Functional
CHEMBL642829
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Evaluated in an functional alpha-v beta-3 antagonism assay, involving adhesion of beta-3-transfected 293 cells to fibrinogen (alpha-v beta-3 293 beta3)
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | HEK293 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Expert |
Publication
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.12 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL127133 | — | — | 1 | 7.77 |
| CHEMBL339751 | — | — | 1 | 7.50 |
| CHEMBL435806 | — | — | 1 | 7.47 |
| CHEMBL127525 | — | — | 1 | 7.47 |
| CHEMBL338806 | — | — | 1 | 7.39 |
| CHEMBL338439 | — | — | 1 | 7.31 |
| CHEMBL338865 | — | — | 1 | 7.25 |
| CHEMBL126341 | — | — | 1 | 7.24 |
| CHEMBL340309 | — | — | 1 | 7.24 |
| CHEMBL338665 | — | — | 1 | 7.13 |
| CHEMBL126071 | — | — | 1 | 7.06 |
| CHEMBL127492 | — | — | 1 | 7.03 |
| CHEMBL339476 | — | — | 1 | 6.97 |
| CHEMBL126983 | — | — | 1 | 6.89 |
| CHEMBL126925 | — | — | 1 | 6.89 |
| CHEMBL127377 | — | — | 1 | 6.80 |
| CHEMBL340703 | — | — | 1 | 6.77 |
| CHEMBL126416 | — | — | 1 | 6.75 |
| CHEMBL419795 | — | — | 1 | 6.36 |
| CHEMBL2111839 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL127133 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL339751 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL435806 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL127525 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL338806 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL338439 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL338865 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL126341 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL340309 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL338665 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL126071 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL127492 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL339476 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL126983 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL126925 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL127377 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL340703 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL126416 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL419795 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL2111839 | — | IC50 | > | 1000.0 | nM | - |