Assay Detail
Binding
CHEMBL3707783
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro Competitive Displacement Binding Assays : Modified SMAC peptides and compounds were tested for their ability to displace the fluorescent tracer from either XIAP, clAP-1 or clAP-2. BIR3 domains of clAP-1 , clAP-2 and XIAP were incubated with test compounds or SMAC based peptides and their respective peptide probes (Peptide Protein Research) in assay buffer (50mM Hepes pH 7.5, 0.025% Tween-20, 0.01 % BSA, and 1 mM DTT). Positive controls consisted of BIR3 proteins and tracer (no inhibition) and negative controls contained tracer only (100% inhibition). The samples were incubated at room temperature for 1 hr (XIAP and clAP-2) or 3hrs (clAP-1 ) prior to being read in the BMG Pherastar in Fluorescence Polarization mode (FP 485nm, 520nm, 520nm).
162
Total Activities
162
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Bicyclic heterocycle compounds and their uses in therapy
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 162 | 6.56 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3699960 | — | — | 1 | 8.05 |
| CHEMBL3700091 | — | — | 1 | 8.02 |
| CHEMBL3600717 | — | — | 1 | 8.00 |
| CHEMBL3700047 | — | — | 1 | 7.96 |
| CHEMBL3700050 | — | — | 1 | 7.96 |
| CHEMBL3700057 | — | — | 1 | 7.96 |
| CHEMBL3699967 | — | — | 1 | 7.92 |
| CHEMBL3700023 | — | — | 1 | 7.92 |
| CHEMBL3699980 | — | — | 1 | 7.92 |
| CHEMBL3700040 | — | — | 1 | 7.89 |
| CHEMBL3700105 | — | — | 1 | 7.85 |
| CHEMBL3700060 | — | — | 1 | 7.85 |
| CHEMBL3700016 | — | — | 1 | 7.85 |
| CHEMBL3700028 | — | — | 1 | 7.85 |
| CHEMBL3699975 | — | — | 1 | 7.85 |
| CHEMBL3700042 | — | — | 1 | 7.85 |
| CHEMBL3699981 | — | — | 1 | 7.85 |
| CHEMBL3700085 | — | — | 1 | 7.85 |
| CHEMBL3700080 | — | — | 1 | 7.85 |
| CHEMBL3699958 | — | — | 1 | 7.80 |
| CHEMBL3699970 | — | — | 1 | 7.80 |
| CHEMBL3699959 | — | — | 1 | 7.80 |
| CHEMBL3699951 | — | — | 1 | 7.77 |
| CHEMBL3699978 | — | — | 1 | 7.77 |
| CHEMBL3700025 | — | — | 1 | 7.77 |
| CHEMBL3700104 | — | — | 1 | 7.77 |
| CHEMBL3700051 | — | — | 1 | 7.75 |
| CHEMBL3700029 | — | — | 1 | 7.72 |
| CHEMBL3699972 | — | — | 1 | 7.72 |
| CHEMBL3639988 | — | — | 1 | 7.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3699960 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3700091 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL3600717 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3700057 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3700050 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3700047 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3699967 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3699980 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3700023 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3700040 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3700028 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700085 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3699981 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700042 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3699975 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700105 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700080 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700016 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3700060 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3699959 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3699970 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3699958 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3699951 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3699978 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3700104 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3700025 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3700051 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3700029 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3699972 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3700094 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3700089 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3639988 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3700079 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3699987 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3700067 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3699979 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3699968 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3700090 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3700106 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3700081 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3699962 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3700061 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3700001 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3700055 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3700058 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3699963 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3699991 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3699961 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL3700059 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3700108 | — | IC50 | = | 41.0 | nM | 7.39 |