Assay Detail
Binding
CHEMBL5738964
Review assay metadata, readout intent, target linkage, and publication context from the same page.
EnPlex (purified enzyme activity assay): This assay is described in Bachovchin et al. Nature Chemical Biology 10, 656-663 (2014). Briefly, purified enzymes are coupled to Luminex microspheres, with a different bead color for each enzyme. Multiplexed bead complexes are incubated with a compound before being treated with a biotinylated activity-based probe and a streptavidin R-phycoerythrin conjugate (SAPE). The mixtures are scanned on a Luminex flow cytometer, where one laser detects the bead color (enzyme identity) and a second laser detects the R-phycoerythrin signal (enzyme activity). The enzyme concentration is calculated assuming 100% of the protein was coupled to the beads.
150
Total Activities
49
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Combination therapies using caspase-1 dependent anticancer agents and PGE2 antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 6.82 | 7.54 |
| kon | 50 | - | - |
| k_off | 50 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63895 | — | — | 3 | 7.54 |
| CHEMBL6059875 | — | — | 3 | 7.51 |
| CHEMBL5993643 | — | — | 3 | 7.48 |
| CHEMBL63860 | — | — | 6 | 7.37 |
| CHEMBL5848496 | — | — | 3 | 7.24 |
| CHEMBL5968328 | — | — | 3 | 7.06 |
| CHEMBL5790536 | — | — | 3 | 6.19 |
| CHEMBL5925037 | — | — | 3 | 5.92 |
| CHEMBL5918829 | — | — | 3 | 5.66 |
| CHEMBL1814633 | — | — | 3 | 5.66 |
| CHEMBL5817549 | — | — | 3 | - |
| CHEMBL6014994 | — | — | 3 | - |
| CHEMBL5980162 | — | — | 3 | - |
| CHEMBL5778991 | — | — | 3 | - |
| CHEMBL5809136 | — | — | 3 | - |
| CHEMBL363250 | — | — | 3 | - |
| CHEMBL63652 | — | — | 3 | - |
| CHEMBL63698 | — | — | 3 | - |
| CHEMBL63726 | — | — | 3 | - |
| CHEMBL3686736 | — | — | 3 | - |
| CHEMBL6055810 | — | — | 3 | - |
| CHEMBL5892398 | — | — | 3 | - |
| CHEMBL5846428 | — | — | 3 | - |
| CHEMBL5994541 | — | — | 3 | - |
| CHEMBL5925489 | — | — | 3 | - |
| CHEMBL5791516 | — | — | 3 | - |
| CHEMBL5768759 | — | — | 3 | - |
| CHEMBL6059646 | — | — | 3 | - |
| CHEMBL494497 | — | — | 3 | - |
| CHEMBL5766821 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63895 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL6059875 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5993643 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL63860 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL63860 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5848496 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5968328 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5790536 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5925037 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1814633 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5918829 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5791516 | — | IC50 | = | 41070.0 | nM | - |
| CHEMBL63652 | — | kon | = | - | — | - |
| CHEMBL5791516 | — | kon | = | - | — | - |
| CHEMBL5791516 | — | k_off | = | - | s-1 | - |
| CHEMBL5925489 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5925489 | — | kon | = | - | — | - |
| CHEMBL5925489 | — | k_off | = | - | s-1 | - |
| CHEMBL5994541 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5994541 | — | kon | = | - | — | - |
| CHEMBL5994541 | — | k_off | = | - | s-1 | - |
| CHEMBL5846428 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5846428 | — | kon | = | - | — | - |
| CHEMBL5846428 | — | k_off | = | - | s-1 | - |
| CHEMBL63698 | — | k_off | = | - | s-1 | - |
| CHEMBL63895 | — | kon | = | - | — | - |
| CHEMBL63726 | — | k_off | = | - | s-1 | - |
| CHEMBL63726 | — | kon | = | - | — | - |
| CHEMBL63726 | — | IC50 | = | 82.0 | nM | - |
| CHEMBL63698 | — | IC50 | = | 150.0 | nM | - |
| CHEMBL6060914 | — | kon | = | - | — | - |
| CHEMBL5892398 | — | k_off | = | - | s-1 | - |
| CHEMBL5968423 | — | k_off | = | - | s-1 | - |
| CHEMBL6039540 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6039540 | — | kon | = | - | — | - |
| CHEMBL6039540 | — | k_off | = | - | s-1 | - |
| CHEMBL5874480 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5874480 | — | kon | = | - | — | - |
| CHEMBL5874480 | — | k_off | = | - | s-1 | - |
| CHEMBL6060914 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5768759 | — | k_off | = | - | s-1 | - |
| CHEMBL6060914 | — | k_off | = | - | s-1 | - |
| CHEMBL5766821 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5766821 | — | kon | = | - | — | - |
| CHEMBL5766821 | — | k_off | = | - | s-1 | - |
| CHEMBL6059646 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL6059646 | — | kon | = | - | — | - |
| CHEMBL6059646 | — | k_off | = | - | s-1 | - |
| CHEMBL5768759 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5768759 | — | kon | = | - | — | - |