Assay Detail
Binding
CHEMBL2066545
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 5-FAM-conjugated AVP-diPhe-FAM from MLXBIR3SG after 30 mins by fluorescence polarization-based competition assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.29 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2063869 | GDC-0152 | 1.0 | 1 | 7.85 |
| CHEMBL2063868 | — | — | 1 | 7.80 |
| CHEMBL2063862 | — | — | 1 | 7.52 |
| CHEMBL2063863 | — | — | 1 | 7.52 |
| CHEMBL2063866 | — | — | 1 | 7.16 |
| CHEMBL2063865 | — | — | 1 | 7.10 |
| CHEMBL2063867 | — | — | 1 | 7.05 |
| CHEMBL2063864 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2063869 | GDC-0152 | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2063868 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2063862 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2063863 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL2063866 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL2063865 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL2063867 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL2063864 | — | Ki | = | 460.0 | nM | 6.34 |