Assay Detail
Binding
CHEMBL2162883
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 6.10 | 7.59 |
| IC50 | 3 | 5.80 | 6.65 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158053 | — | — | 1 | 7.59 |
| CHEMBL2158051 | XEVINAPANT | 3.0 | 2 | 7.18 |
| CHEMBL365059 | — | — | 2 | 5.45 |
| CHEMBL2158052 | — | — | 2 | 4.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158053 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL2158051 | XEVINAPANT | Ki | = | 66.4 | nM | 7.18 |
| CHEMBL2158051 | XEVINAPANT | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL365059 | — | Ki | = | 3535.0 | nM | 5.45 |
| CHEMBL365059 | — | IC50 | = | 11584.0 | nM | 4.94 |
| CHEMBL2158052 | — | Ki | = | 67300.0 | nM | 4.17 |
| CHEMBL2158052 | — | IC50 | = | 221000.0 | nM | - |