Assay Detail
Binding
CHEMBL3889108
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Fluorescence Polarization Assay: Assays were performed in black, flat-bottom, 384-well plates. The final assay volume was 50 μL prepared from additions of N-His-Tb-BIR3(241-356, XIAP), fluoresceinated modified SMAC peptide, and test compounds in assay buffer consisting of 20 mM Sodium Phosphate, 1 mM EDTA, 50 mM NaCl, and 0.05% PLURONIC® F68. The reaction was incubated at room temperature for 60 minutes and fluorescence polarization of the reaction was detected on the LJL Plate Reader Inhibition data were calculated from mP values generated by the no protein control reactions for 100% inhibition and vehicle-only reactions for 0% inhibition. The final concentration of reagents in the assay was 130 nM N-His-Tb-BIR3(241-356, XIAP), 1.4 nM fluoresceinated modified SMAC peptide, and 1% DMSO.
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
IAP antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.90 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3918792 | — | — | 1 | 10.22 |
| CHEMBL3929256 | — | — | 2 | 10.22 |
| CHEMBL3940255 | — | — | 1 | 10.22 |
| CHEMBL3913296 | — | — | 1 | 10.22 |
| CHEMBL3930765 | — | — | 1 | 10.15 |
| CHEMBL3950036 | — | — | 1 | 10.10 |
| CHEMBL3903824 | — | — | 1 | 10.10 |
| CHEMBL3976012 | — | — | 1 | 9.89 |
| CHEMBL3941276 | — | — | 1 | 9.85 |
| CHEMBL3927714 | — | — | 1 | 9.85 |
| CHEMBL3950322 | — | — | 1 | 9.85 |
| CHEMBL3940832 | — | — | 2 | 9.82 |
| CHEMBL3896723 | — | — | 1 | 9.80 |
| CHEMBL3917007 | — | — | 1 | 9.74 |
| CHEMBL3946177 | — | — | 1 | 9.68 |
| CHEMBL3918274 | — | — | 1 | 9.66 |
| CHEMBL3954865 | — | — | 1 | 9.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3918792 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3940255 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3929256 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3913296 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL3930765 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL3950036 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3903824 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL3976012 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL3950322 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3941276 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3927714 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL3940832 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL3896723 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL3917007 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3946177 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL3918274 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL3940832 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL3929256 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3954865 | — | IC50 | = | 0.27 | nM | 9.57 |