Assay Detail
Binding
CHEMBL2162884
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of human cIAP1 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 |
Target
Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.86 | 8.72 |
| IC50 | 3 | 6.11 | 7.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2158051 | XEVINAPANT | 3.0 | 2 | 8.72 |
| CHEMBL365059 | — | — | 2 | 6.73 |
| CHEMBL2158052 | — | — | 2 | 5.14 |
| CHEMBL2158053 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2158051 | XEVINAPANT | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2158051 | XEVINAPANT | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL365059 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL365059 | — | IC50 | = | 999.0 | nM | 6.00 |
| CHEMBL2158052 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL2158052 | — | IC50 | = | 38900.0 | nM | 4.41 |
| CHEMBL2158053 | — | Ki | < | 1.0 | nM | - |