Assay Detail
Binding
CHEMBL1776950
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Competitive inhibition of His-tagged human XIAP BIR3 domain expressed in Escherichia coli BL21(DE3) after 2 to 3 hrs by fluorescence polarization assay
16
Total Activities
16
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
Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.57 | 6.88 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1774160 | — | — | 1 | 6.88 |
| CHEMBL1774031 | — | — | 1 | 6.87 |
| CHEMBL1774154 | — | — | 1 | 6.82 |
| CHEMBL1774161 | — | — | 1 | 6.79 |
| CHEMBL1774158 | — | — | 1 | 6.75 |
| CHEMBL1774157 | — | — | 1 | 6.73 |
| CHEMBL1774156 | — | — | 1 | 6.72 |
| CHEMBL1774163 | — | — | 1 | 6.67 |
| CHEMBL1774162 | — | — | 1 | 6.67 |
| CHEMBL1774164 | — | — | 1 | 6.55 |
| CHEMBL1773083 | — | — | 1 | 6.37 |
| CHEMBL1774165 | — | — | 1 | 6.28 |
| CHEMBL1774159 | — | — | 1 | 6.21 |
| CHEMBL1774166 | — | — | 1 | 6.21 |
| CHEMBL481422 | — | — | 1 | 6.09 |
| CHEMBL1774155 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1774160 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL1774031 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL1774154 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL1774161 | — | IC50 | = | 161.0 | nM | 6.79 |
| CHEMBL1774158 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL1774157 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL1774156 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL1774163 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL1774162 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL1774164 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1773083 | — | IC50 | = | 426.0 | nM | 6.37 |
| CHEMBL1774165 | — | IC50 | = | 523.0 | nM | 6.28 |
| CHEMBL1774159 | — | IC50 | = | 613.0 | nM | 6.21 |
| CHEMBL1774166 | — | IC50 | = | 618.0 | nM | 6.21 |
| CHEMBL481422 | — | IC50 | = | 819.0 | nM | 6.09 |
| CHEMBL1774155 | — | IC50 | > | 50000.0 | nM | - |