Assay Detail
Binding
CHEMBL4015173
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Antagonist activity at integrin alphaVbeta3 (unknown origin) expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen after 2 hrs by MTT assay
8
Total Activities
8
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
New potent and selective αvβ3 integrin ligands: Macrocyclic peptides containing RGD motif synthesized by sortase A-mediated ligation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.15 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL429876 | CILENGITIDE | 3.0 | 1 | 6.66 |
| CHEMBL4079738 | — | — | 1 | 5.14 |
| CHEMBL4085518 | — | — | 1 | 4.48 |
| CHEMBL4097763 | — | — | 1 | 4.31 |
| CHEMBL4068971 | — | — | 1 | - |
| CHEMBL4090048 | — | — | 1 | - |
| CHEMBL4067904 | — | — | 1 | - |
| CHEMBL141005 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL429876 | CILENGITIDE | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4079738 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4085518 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4097763 | — | IC50 | = | 48800.0 | nM | 4.31 |
| CHEMBL4068971 | — | IC50 | = | 257000.0 | nM | - |
| CHEMBL4090048 | — | IC50 | = | 171000.0 | nM | - |
| CHEMBL4067904 | — | IC50 | = | 152000.0 | nM | - |
| CHEMBL141005 | — | IC50 | = | 619000.0 | nM | - |